Claims Analysis
Total Claims: 18
Claim 1
Independent Claim
731 words
A compound of the formula ##STR153## wherein Y 1 is chloro, Y 2 is OR and Y 3 is hydrogen or OR and the pharmaceutically acceptable acid addition salts thereof; R is alkyl having from one to three carbon atoms; R 1 and R 2 are the same or different and when taken separately are each a member selected from the group consisting of hydrogen, alkyl having from 1 to 5 carbon atoms, cycloalkyl having from 3 to 8 carbon atoms; alkenyl having from 3 to 5 carbon atoms, alkynyl having from 3 to 5 carbon atoms, hydroxy substituted alkyl having from 2 to 5 carbon atoms and when taken together with the nitrogen atom to which they are attached R 1 and R 2 form ##STR154## where X 1 is a member selected from the group consisting of S(O) t , CHOR 6 , --(CH 2 ) p -- and CHR 7 , and X 2 is a member selected from the group consisting of X 1 , O, NR 3 , NCOR 4 and NCOOR 5 , where m is 2 or 3, n is 2 or 3, p is 1 to 3, t is 0, 1 or 2; R 3 is a member selected from the group consisting of hydrogen, alkyl having from 1 to 6 carbon atoms, alkenyl from 3 to 5 carbon atoms, alkynyl having from 3 to 5 carbon atoms, hydroxy substituted alkyl having from 2 to 5 carbon atoms, cycloalkyl having from 3 to 8 carbon atoms, --(CH 2 ) q C 6 H 4 R 8 and --(CH 2 ) q C 10 H 6 R 8 , where q is 0 or 1; R 4 is a member selected from the group consisting of hydrogen, alkyl having from 1 to 6 carbon atoms, alkenyl having from 3 to 5 carbon atoms, cycloalkyl and cycloalkylmethyl wherein said cycloalkyl has from 3 to 8 carbon atoms, ##STR155## R 10 , CH 2 R 10 and (CH 2 ) q C 6 H 4 R 8 where A is S or O, q is as defined above and R 10 is a member selected from the group consisting of ##STR156## where r is 1 or 2; R 5 is a member selected from the group consisting of alkyl having from 1 to 7 carbon atoms, alkenyl having 3 to 5 carbon atoms, cycloalkyl having from 3 to 8 carbon atoms, hydroxy substituted alkyl having from 2 to 5 carbon atoms, CH 2 C 6 H 4 R 8 , CH 2 C 10 H 6 R 8 , CH 2 R 10 and CH 2 O-pyridyl; R 6 is a member selected from the group consisting of hydrogen, C 6 H 4 R 8 , --(CH 2 ) p Z R 15 , alkyl having from 1 to 6 carbon atoms and said alkyl substituted by a member selected from the group consisting of Cl, F, Br, OH, CH 3 O, SO 2 CH 3 and NHSO 2 CH 3 , where p and A are as previously defined and Z is a member selected from the group consisting of O, S, SO, SO 2 , and NR 16 ; R 7 is a member selected from the group consisting of alkyl having from one to six carbon atoms, hydroxyalkyl having from one to five carbon atoms, --(CH 2 ) q C 6 H 4 R 8 and COC 6 H 4 R 8 ; R 8 is a member selected from the group consisting of H, Cl, Br, F, CH 3 , CH 3 O, CF 3 , OH, SO 2 CH 3 and NHSO 2 CH 3 ; R 9 is a member selected from the group consisting of H, Cl, CH 3 , C 2 H 5 and phenyl; R 11 is hydrogen or methylthio and R 12 is a member selected from the group consisting of H, NH 2 alkyl having from one to four carbon atoms and NHCO 2 R 14 ; R 14 is alkyl having from one to four carbon atoms; R 15 is a member selected from the group consisting of alkyl having from one to four carbon atoms, C 6 H 4 R 8 and C 10 H 6 R 8 ; and R 16 is hydrogen or alkyl having from one to four carbon atoms.
Claim 2
Dependent Claim
731 words
A compound of the formula ##STR153## wherein Y 1 is chloro, Y 2 is OR and Y 3 is hydrogen or OR and the pharmaceutically acceptable acid addition salts thereof; R is alkyl having from one to three carbon atoms; R 1 and R 2 are the same or different and when taken separately are each a member selected from the group consisting of hydrogen, alkyl having from 1 to 5 carbon atoms, cycloalkyl having from 3 to 8 carbon atoms; alkenyl having from 3 to 5 carbon atoms, alkynyl having from 3 to 5 carbon atoms, hydroxy substituted alkyl having from 2 to 5 carbon atoms and when taken together with the nitrogen atom to which they are attached R 1 and R 2 form ##STR154## where X 1 is a member selected from the group consisting of S(O) t , CHOR 6 , --(CH 2 ) p -- and CHR 7 , and X 2 is a member selected from the group consisting of X 1 , O, NR 3 , NCOR 4 and NCOOR 5 , where m is 2 or 3, n is 2 or 3, p is 1 to 3, t is 0, 1 or 2; R 3 is a member selected from the group consisting of hydrogen, alkyl having from 1 to 6 carbon atoms, alkenyl from 3 to 5 carbon atoms, alkynyl having from 3 to 5 carbon atoms, hydroxy substituted alkyl having from 2 to 5 carbon atoms, cycloalkyl having from 3 to 8 carbon atoms, --(CH 2 ) q C 6 H 4 R 8 and --(CH 2 ) q C 10 H 6 R 8 , where q is 0 or 1; R 4 is a member selected from the group consisting of hydrogen, alkyl having from 1 to 6 carbon atoms, alkenyl having from 3 to 5 carbon atoms, cycloalkyl and cycloalkylmethyl wherein said cycloalkyl has from 3 to 8 carbon atoms, ##STR155## R 10 , CH 2 R 10 and (CH 2 ) q C 6 H 4 R 8 where A is S or O, q is as defined above and R 10 is a member selected from the group consisting of ##STR156## where r is 1 or 2; R 5 is a member selected from the group consisting of alkyl having from 1 to 7 carbon atoms, alkenyl having 3 to 5 carbon atoms, cycloalkyl having from 3 to 8 carbon atoms, hydroxy substituted alkyl having from 2 to 5 carbon atoms, CH 2 C 6 H 4 R 8 , CH 2 C 10 H 6 R 8 , CH 2 R 10 and CH 2 O-pyridyl; R 6 is a member selected from the group consisting of hydrogen, C 6 H 4 R 8 , --(CH 2 ) p Z R 15 , alkyl having from 1 to 6 carbon atoms and said alkyl substituted by a member selected from the group consisting of Cl, F, Br, OH, CH 3 O, SO 2 CH 3 and NHSO 2 CH 3 , where p and A are as previously defined and Z is a member selected from the group consisting of O, S, SO, SO 2 , and NR 16 ; R 7 is a member selected from the group consisting of alkyl having from one to six carbon atoms, hydroxyalkyl having from one to five carbon atoms, --(CH 2 ) q C 6 H 4 R 8 and COC 6 H 4 R 8 ; R 8 is a member selected from the group consisting of H, Cl, Br, F, CH 3 , CH 3 O, CF 3 , OH, SO 2 CH 3 and NHSO 2 CH 3 ; R 9 is a member selected from the group consisting of H, Cl, CH 3 , C 2 H 5 and phenyl; R 11 is hydrogen or methylthio and R 12 is a member selected from the group consisting of H, NH 2 alkyl having from one to four carbon atoms and NHCO 2 R 14 ; R 14 is alkyl having from one to four carbon atoms; R 15 is a member selected from the group consisting of alkyl having from one to four carbon atoms, C 6 H 4 R 8 and C 10 H 6 R 8 ; and R 16 is hydrogen or alkyl having from one to four carbon atoms.
Claim 3
Dependent Claim
16 words
A compound according to claim 1 wherein Y 3 is hydrogen and Y 2 is methoxy.
Claim 4
Dependent Claim
15 words
A compound according to claim 1 wherein Y 2 and Y 3 are each methoxy.
Claim 5
Dependent Claim
25 words
A compound according to claim 1 wherein R 1 and R 2 taken together with the nitrogen atom to which they are attached form ##STR157##
Claim 6
Dependent Claim
37 words
A compound according to claim 4 wherein R 4 is a member of the group consisting of ##STR158## and cycloalkyl having from 3 to 8 carbon atoms and A, r and R 11 are as previously defined.
Claim 7
Dependent Claim
11 words
A compound according to claim 5 wherein R 4 is 2-furyl.
Claim 8
Dependent Claim
25 words
A compound according to claim 1 wherein R 1 and R 2 taken together with the nitrogen atom to which they are attached form ##STR159##
Claim 9
Dependent Claim
20 words
A compound according to claim 7 wherein R 5 is hydroxy substituted alkyl having from 2 to 5 carbon atoms.
Claim 10
Dependent Claim
11 words
A compound according to claim 8 wherein R 5 is 2-methyl-2-hydroxypropyl.
Claim 11
Dependent Claim
7 words
The compound according to claim 1: 2-[4-(2-furoyl)-1-piperazinyl]-4-amino-6-chloro-7-methoxyquinazoline.
Claim 12
Dependent Claim
7 words
The compound according to claim 1: 2-[4-(2-hydroxy-2-methylprop-1-yloxycarbonyl)piperazin-1-yl]-4-amino-6-chloro-7-methoxyquinazoline.
Claim 13
Dependent Claim
28 words
A pharmaceutical composition for oral or parenteral administration to a mammal comprising a pharmaceutically acceptable carrier and an antihypertensive effective amount of a compound according to claim 1.
Claim 14
Dependent Claim
11 words
The composition according to claim 12 wherein said compound is 2-[4-(2-furoyl)-1-piperazinyl]-4-amino-6-chloro-7-methoxyquinazoline.
Claim 15
Dependent Claim
11 words
The composition according to claim 12 wherein said compound is 2-[4-(2-hydroxy-2-methylprop-1-yloxycarbonyl)piperazin-1-yl]-4-amino-6-chloro-7-methoxyquinazoline.
Claim 16
Dependent Claim
30 words
A method for treating hypertension which comprises orally or parenterally administering to a mammal in need of such treatment an antihypertensive effective amount of a compound according to claim 1.
Claim 17
Dependent Claim
11 words
The method according to claim 15 wherein said compound is 2-[4-(2-furoyl)-1-piperazinyl]-4-amino-6-chloro-7-methoxyquinazoline.
Claim 18
Dependent Claim
11 words
The method according to claim 15 wherein said compound is 2-[4-(2-hydroxy-2-methylprop-1-yloxycarbonyl)piperazin-1-yl]-4-amino-6-chloro-7-methoxyquinazoline.