Diacyl-substituted guanidines, a process for their...

Details Diacyl-substituted guanidines, a process for their... Diacyl-substituted guanidines, a process for their...

1997-04-18

2002-08-20

Davis, Brian J. (Department: 1621)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Nitrogen containing other than solely as a nitrogen in an...

C514S311000, C514S331000, C514S351000, C514S397000, C514S399000, C514S427000, C514S428000, C514S594000, C546S168000, C546S169000, C546S175000, C546S231000, C546S332000, C548S313700, C548S314400, C548S340100, C548S561000, C548S566000, C564S050000, C564S051000, C564S225000, C564S230000, C564S237000

Reexamination Certificate

active

06436999

ABSTRACT:

The invention relates to diacyl-substituted guanidines of the formula I
in which:
X(1) and X(2) are
T1 is zero, 1, 2, 3 or 4,
R(A) and R(B) are, independently,
 hydrogen, F, Cl, Br, I, CN, OR(106), (C
1
-C
8
)-alkyl, (C
3
-C
8
)-cycloalkyl, O
zk
(CH
2
)
zl
C
zm
F
2zm+1
, NR(107)R(108), phenyl or benzyl,
where the aromatic radicals are not substituted or are substituted by 1-3 substituents selected from the group consisting of F, Cl, CF
3
, methyl, methoxy and NR(109)R(110),
R(109) and R(110) being
 hydrogen, (C
1
-C
4
)-alkyl or (C
1
-C
4
)-perfluoroalkyl,
 zl is zero, 1, 2, 3 or 4,
 zk is zero or 1,
 zm is 1, 2, 3, 4, 5, 6, 7 or 8,
 R(106) is
hydrogen, (C
1
-C
8
)-alkyl, (C
1
-C
8
)-perfluoroalkyl, (C
3
-C
8
)-alkenyl, (C
3
-C
8
)-cycloalkyl, phenyl or benzyl,
 where the aromatic radicals are not substituted or are substituted by 1-3 substituents selected from the group consisting of F, Cl, CF
3
, methyl, methoxy and NR(111)R(112),
 R(111) and R(112) being
hydrogen, (C
1
-C
4
)-alkyl or (C
1
-C
4
)-perfluoroalkyl,
 R(107) and R(108) are, independently of each other, defined as R(106),
 or
 R(107) and R(108) are together 4 or 5 methylene groups of which one CH
2
group can be replaced by oxygen, S, NH, N—CH
3
or N-benzyl,
or
X(1) and X(2) are
 T2a and T2b are, independently of each other, zero, 1 or 2,
 where the double bond can have the E or Z configuration;
or
X(1) and X(2) are
T3 is zero, 1 or 2,
U, YY and Z are, independently of each other,
 C or N,
 where U, YY and Z can carry the following number of substituents:
Bonded to a double
Number of permitted
U, YY or Z
bond in the ring
substituents
C
yes
1
C
no
2
N
yes
0
N
no
1
R(D) is hydrogen, (C
1
-C
8
)-alkyl or (C
1
-C
8
)-perfluoroalkyl, R(U1), R(U2), R(Y1), R(Y2), R(Z1) and R(Z2) are, independently of each other,
 hydrogen, F, Cl, Br, I, CN, OR(114), (C
1
-C
8
)-alkyl, (C
3
-C
8
)-cycloalkyl, O
zka
(CH
2
)
zla
C
zma
F
2zma+1
,
 NR(115)R(116), phenyl or benzyl,
where the aromatic radicals are not substituted or are substituted by 1-3 substituents selected from the group consisting of F, Cl, CF
3
, methyl, methoxy and NR(117)R(118),
 R(117) and R(118) being
hydrogen, (C
1
-C
4
)-alkyl or (C
1
-C
4
) perfluoroalkyl,
zka is zero or 1,
zla is zero, 1, 2, 3 or 4,
zma is 1, 2, 3, 4, 5, 6, 7 or 8,
R(114) is hydrogen, (C
1
-C
8
)-alkyl, (C
1
-C
8
)-perfluoroalkyl, (C
3
-C
8
)-alkenyl, (C
3
-C
8
)-cycloalkyl, phenyl or benzyl,
 where the aromatic radicals are not substituted or are substituted by 1-3 substituents selected from the group consisting of F, Cl, CF
3
, methyl, methoxy and NR(119)R(120),
 R(119) and R(120) being
hydrogen, (C
1
-C
4
)-alkyl or (C
1
-C
4
)-perfluoroalkyl,
R(115) and R(116) are, independently of each other, defined as R(114),
or
R(115) and R(116)
 are together 4 or 5 methylene groups of which one CH
2
group can be replaced by oxygen, S, NH, N—CH
3
or N-benzyl,
 where, however, the constitution U is nitrogen (N), YY is nitrogen (N) and Z is carbon (C) is excepted,
R(101), R(102), R(103), R(104) and R(105) are, independently of each other,
 hydrogen, F, Cl, Br, I, —C≡N, X
zoa
—(CH
2
)
zpa
—(C
zqa
F
2zqa+1
), R(110a)—SO
zbm
, R(110b)R(110c)N—CO, R(111a)—CO— or R(112a)R(113a)N—SO
2
—,
where the perfluoroalkyl group is straight-chain or branched,
 X is hydrogen, S or NR(114a),
 zoa is zero or 1,
 R(114a) being H or (C
1
-C
3
)-alkyl,
 zbm is zero, 1 or 2,
 zpa is zero, 1, 2, 3 or 4,
 zqa is 1, 2, 3, 4, 5, 6, 7 or 8,
 R(110a), R(110b), R(111a) and R(112a) are, independently,
(C
1
-C
8
)-alkyl, (C
3
-C
8
)-alkenyl, —C
zn
H
2zn
—R(115a) or (C
1
-C
8
)-perfluoroalkyl,
zn is zero, 1, 2, 3 or 4,
 R(115a) is
(C
3
-C
8
)-cycloalkyl, phenyl, biphenylyl or naphthyl,
 where the aromatic radicals are not substituted or are substituted by 1-3 substituents selected from the group consisting of F, Cl, CF
3
, methyl, methoxy and NR(116a)R(117a),
 R(116a) and R(117a) being
hydrogen, (C
1
-C
4
)-perfluoroalkyl or (C
1
-C
4
)-alkyl,
 or
 R(110b), R(111a) and R(112a) are also hydrogen,
 R(110c) and R(113a) are, independently,
hydrogen, (C
1
-C
4
)-perfluoroalkyl or (C
1
-C
4
)-alkyl,
 or
 R(110b) and R(110c) and also R(112a) and R(113a) are together 4 or 5 methylene groups, of which one CH
2
group can be replaced by oxygen, sulfur, NH, N—CH
3
or N-benzyl,
or
R(101), R(102), R(103), R(104) and R(105) are, independently of each other,
 (C
1
-C
8
)-alkyl, —C
za
H
2zal
R(118a) or (C
3
-C
8
)-alkenyl,
 zal is zero, 1, 2, 3 or 4,
 R(118a) is
(C
3
-C
8
)-cycloalkyl, phenyl, biphenylyl or naphthyl,
 where the aromatic radicals are not substituted or are substituted by 1-3 substituents from the group consisting of F, Cl, CF
3
, methyl, methoxy or NR(119a)R(119b),
 R(119a) and R(119b) being
hydrogen, (C
1
-C
4
)-alkyl or (C
1
-C
4
)-perfluoroalkyl,
or
R(101), R(102), R(103), R(104) and R(105) are, independently of each other,
 (C
1
-C
9
)-heteroaryl which is linked via C or N and which is unsubstituted or is substituted by 1-3 substituents from the group consisting of F, Cl, CF
3
, CH
3
, methoxy, hydroxyl, amino, methylamino and dimethylamino,
or
R(101), R(102), R(103), R(104) and R(105) are, independently of each other,
 —C≡C—R(193),
 R(193) is
phenyl which is not substituted or is substituted by 1-3 substituents from the group consisting of F, Cl, CF
3
, methyl, methoxy or NR(194)R(195),
R(194) and R(195) being
 hydrogen or CH
3
,
or
R(101), R(102), R(103), R(104) and R(105) are, independently of each other,
 —Y-para-C
6
H
4
—(CO)
zh
—(CHOH)
zi
—(CH
2
)
zj
—(CHOH)
zk
—R(123), —Y-meta-C
6
H
4
—(CO)
zad
—(CHOH)
zae
—(CH
2
)
zaf
—(CHOH)
zag
—R(124)
 or
 —Y-ortho-C
6
H
4
—(CO)
zah
—(CHOH)
zao
—(CH
2
)
zap
—(CHOH)
zak
—R(125),
 Y is oxygen, —S— or —NR(122d)—,
 zh, zad and zah are, independently,
zero or 1,
 zi, zj, zk, zae, zaf, zag, zao, zap and zak are, independently,
zero, 1, 2, 3 or 4,
 where, however, in each case,
zh, zi and zk are not simultaneously zero, zad, zae and zag are not simultaneously zero and zah, zao and zak are not simultaneously zero,
 R(123), R(124) R(125) and R(122d) are, independently, hydrogen or (C
1
-C
3
)-alkyl,
or
R(101), R(102), R(103), R(104) and R(105) are, independently of each other,
 SR(129), —OR(130), —NR(131)R(132) or —CR(133)—R(134)R(135),
 R(129), R(130), R(131) and R(133), are, independently,
—C
zab
H
2zab
—(C
1
-C
9
)-heteroaryl which is unsubstituted or is substituted by 1-3 substituents from the group consisting of F, Cl, CF
3
, CH
3
, methoxy, hydroxyl, amino, methylamino and dimethylamino,
zab is zero, 1 or 2,
 R(132), R(134) and R(135) are, independently of each other,
defined as R(129), or hydrogen, (C
1
-C
4
)-alkyl or (C
1
-C
4
)-perfluoroalkyl,
or
R(101), R(102), R(103), R(104) and R(105) are, independently of each other,
 —W-para-(C
6
H
4
)—R(196), —W-meta-(C
6
H
4
)—R(197) or —W-ortho-(C
6
H
4
)—R(198),
 R(196), R(197) and R(198) are, independently,
(C
1
-C
9
)-heteroaryl which is linked via C or N and which is unsubstituted or is substituted by 1 to 3 substituents from the group consisting of F, Cl, CF
3
, CH
3
, methoxy, hydroxyl, amino, methylamino, dimethylamino and benzyl,
W is oxygen, S or NR(136)—,
R(136) being hydrogen or (C
1
-C
4
)-alkyl,
or
R(101), R(102), R(103), R(104) and R(105) are, independently of each other,
 R(146)X(1a)—,
 X(1a) is oxygen, S, NR(147), (D═O)A— or NR(148)C═MN
(*)
R(149)—,
M is oxygen or sulfur,
A is oxygen or NR(150), and
D is C or SO,
 R(146) is (C
1
-C
8
)-alkyl, (C
3
-C
8
)-alkenyl, (CH
2
)
zbz
C
zdz
F
2zdz+1
or —C
zxa
H
2zxa
—R(151),
zbz is zero or 1,
zdz is 1, 2, 3, 4, 5, 6 or 7,
zxa is zero, 1, 2, 3 or 4,
R(151) is
 (C
3
-C
8
)-cycloalkyl, phenyl, biphenylyl or naphthyl,
 where the aromatic radicals are not substituted or are substituted by 1-3 substituents from the group consisti

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