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US 5,633,277 AGranted
Sulfonamide aminomethylene derivatives as immunosuppressants
AssigneeMiles Inc.
InventorsRichard D. Connell, David G. Osterman, Michael E. Katz, Robert D. Dally
Life of this patent
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Abstract
Compounds which suppress human T-lymphocyte proliferation are disclosed. The active compounds essentially contain at least the following structure: ##STR1##
Claims12
A compound having the structure:
- ##STR32## where R.sup.0 is straight or branched (C.sub.1 -C.sub.10)alkyl, (C.sub.3 -C.sub.10)cycloalkyl, (C.sub.5 -C.sub.12)bicycloalkyl, or (C.sub.7 -C.sub.14)tricycloalkyl, each of which is optionally substituted with a straight or branched (C.sub.1 -C.sub.3)alkoxy, cyano, straight or branched carbo(C.sub.1 -C.sub.6)alkoxy, (C.sub.1 -C.sub.5)alkylsulfonyl, one to three fluoro groups, or with a doubly bonded oxygen atom to form a ketone;
- or R.sup.0 is styryl, or a phenyl group optionally substituted up to three times with a straight or branched (C.sub.1 -C.sub.6)alkyl;
- R.sup.1 is hydrogen or methyl;
- one of R.sup.2 and R.sup.3 is hydrogen and the other is straight or branched (C.sub.1 -C.sub.6)alkyl optionally substituted with C.sub.6 cycloalkyl, hydroxy, straight or branched (C.sub.1 -C.sub.4)alkoxy, benzyloxy, or aryl optionally substituted with hydroxy or methoxy;
- n is the integer 2;
- X.sup.1 is NR.sup.4, where R.sup.4 is hydrogen or methyl;
- J is the divalent fragment ##STR33## where R.sup.5 is hydrogen, or straight or branched (C.sub.1 -C.sub.8)alkyl optionally substituted with hydroxy, straight or branched (C.sub.1 -C.sub.6)alkoxy, benzyloxy, C.sub.6 cycloalkyl or phenyl;
- K is one of the fragments
- --HC.dbd.CH-- or --(CH.sub.2).sub.p --
- where;
- p is the integer 1, 2, 3 or 4;
- and
- L is hydrogen, phenyl, or straight or branched (C.sub.1 -C.sub.8)alkyl optionally substituted with phenyl optionally substituted by straight or branched (C.sub.1 -C.sub.5)alkoxy, hydroxy, or amino, which amino is optionally substituted by a straight or branched (C.sub.1 -C.sub.6)alkyl, acetyl, or both.
10 more elements
A compound having the structure:
- ##STR34## where R.sup.0 is straight or branched (C.sub.1 -C.sub.8)alkyl, (C.sub.3 -C.sub.8)cycloalkyl, (C.sub.5 -C.sub.10)bicycloalkyl, or (C.sub.7 -C.sub.12)tricycloalkyl, each of which is optionally substituted with a fluoro, methoxy, cyano, straight or branched carbo(C.sub.1 -C.sub.4)alkoxy, (C.sub.1 -C.sub.4)alkylsulfonyl or with doubly bonded oxygen to form a ketone;
- or R.sup.0 is styryl, or a phenyl group optionally substituted up to three times by straight or branched (C.sub.1 -C.sub.6)alkyl;
- R.sup.1 is hydrogen or methyl;
- one of R.sup.2 and R.sup.3 is hydrogen and the other is straight or branched (C.sub.1 -C.sub.6) alkyl optionally substituted by C.sub.6 cycloalkyl or phenyl;
- n is the integer 2;
- X.sup.1 is NR.sup.4, where R.sup.4 is hydrogen or methyl;
- J is the divalent fragment ##STR35## where R.sup.5 is hydrogen or straight or branched (C.sub.1 -C.sub.6)alkyl optionally substituted with hydroxy, straight or branched (C.sub.1 -C.sub.6)alkoxy, benzyloxy, C.sub.6 cycloalkyl, or phenyl;
- K is one of the fragments
- --HC.dbd.CH-- or --(CH.sub.2).sub.p --
- where
- p is the integer 2 or 3:
- and
- L is hydrogen, phenyl, or straight or branched (C.sub.1 -C.sub.6)alkyl optionally substituted with phenyl optionally substituted with (C.sub.1 -C.sub.5)alkoxy, hydroxy, or amino, which amino is optionally substituted by (C.sub.1 -C.sub.4)alkyl, or acetyl, or both.
10 more elements
A compound having the structure:
- ##STR36## where R.sup.0 is straight or branched (C.sub.1 -C.sub.6)alkyl optionally substituted with methylsulfonyl;
- or
- R.sup.0 is styryl or a C.sub.10 tricycloalkyl substituted by a doubly bonded oxygen to form a ketone;
- or R.sup.0 is phenyl optionally substituted up to three times by straight or branched (C.sub.1 -C.sub.3)alkyl;
- R.sup.1 is hydrogen;
- one of R.sup.2 and R.sup.3 is hydrogen and the other is straight or branched (C.sub.1 -C.sub.4)alkyl optionally substituted by C.sub.6 cycloalkyl;
- n is the integer 2;
- X.sup.1 is NH;
- J is the divalent fragment ##STR37## where R.sup.5 is hydrogen or straight or branched (C.sub.1 -C.sub.4)alkyl;
- K is one of the fragments
- --HC.dbd.CH-- or --(CH.sub.2).sub.p --
- where
- p is the integer 2;
- and
- L is hydrogen, phenyl, or straight or branched (C.sub.1 -C.sub.3)alkyl optionally substituted by aryl.
12 more elements
Dependencies are inferred from the claim text.