Frances M Nelson

US Patent:

55211941, May 28, 1996

Filed:

May 24, 1995

Appl. No.:

8/450769

Inventors:

Frances C. Nelson - Yardley PA
Guy A. Schiehser - Yardley PA

Assignee:

American Home Products Corporation - Madison NJ

International Classification:

A61K 31395
C07D49516

US Classification:

514291

Abstract:

A compound of the structure ##STR1## wherein R and R. sup. 1 are each independently, ##STR2## or hydrogen; R. sup. 2 and R. sup. 3 are each, independently, alkyl, arylalkyl, or R. sup. 2 and R. sup. 3 may be taken together to form a cycloalkyl ring; R. sup. 4 is a heterocyclic N-oxide radical, which may be optionally substituted; R. sup. 5 is alkyl or arylalkyl; R. sup. 6 and R. sup. 7 are taken together to form a saturated N-alkyl-heterocyclic N-oxide, which may be optionally substituted; k=0-1, m=0-1; n=1-6; with the proviso that R and R. sup. 1 are not both hydrogen, which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.

US Patent:

52567907, Oct 26, 1993

Filed:

Jan 27, 1993

Appl. No.:

8/009605

Inventors:

Frances C. Nelson - Yardley PA

Assignee:

American Home Products Corporation - New York NY

International Classification:

C07D49816
A61K 31695

US Classification:

514291

Abstract:

This invention provides a compound of formula I, ##STR1## and 27-substituted derivatives thereof which are useful as immunosuppressive, antiinflammatory, antifungal, antitumor, and antiproliferative agents. The compound depicted by formula I is named 27-hydroxyrapamycin, and may also be referred to as 27-deoxo-27-hydroxyrapamycin.

US Patent:

55082904, Apr 16, 1996

Filed:

May 24, 1995

Appl. No.:

8/449167

Inventors:

Frances C. Nelson - Yardley PA
Guy A. Schiehser - Yardley PA

Assignee:

American Home Products Corporation - Madison NJ

International Classification:

A61K 31395
C07D49516

US Classification:

514 91

Abstract:

A compound of the structure ##STR1## wherein R and R. sup. 1 are each, independently, ##STR2## or hydrogen; R. sup. 2 and R. sup. 3 are each, independently, alkyl, arylalkyl , or R. sup. 2 and R. sup. 3 may be taken together to form a cycloalkyl ring; R. sup. 4 is a heterocyclic N-oxide radical, which may be optionally substituted; R. sup. 5 is alkyl or arylalkyl; R. sup. 6 and R. sup. 7 are taken together to form a saturated N-alkyl-heterocyclic N-oxide, which may be optionally substituted; k=0-1, m=0-1; n=1-6; with the proviso that R and R. sup. 1 are not both hydrogen, which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.

US Patent:

53026004, Apr 12, 1994

Filed:

Jul 22, 1993

Appl. No.:

8/096071

Inventors:

Frances C. Nelson - Yardley PA

Assignee:

American Home Products Corporation - Madison NJ

International Classification:

C07D49816
A61K 31695

US Classification:

514291

Abstract:

This invention provides a compound of formula I, ##STR1## and 27-substituted derivatives thereof which are useful as immunosuppressive, anti-inflammatory, antifungal, antitumor, and antiproliferative agents. The compound depicted by formula I is named 27-hydroxyrapamycin, and may also be referred to as 27-deoxo-27-hydroxyrapamycin.

US Patent:

53876806, Feb 7, 1995

Filed:

Aug 10, 1993

Appl. No.:

8/105090

Inventors:

Frances C. Nelson - Yardley PA

Assignee:

American Home Products Corporation - Madison NJ

International Classification:

C07D49106
A61K 31395

US Classification:

540456

Abstract:

This invention provides C-22 substituted rapamycin derivatives of the following formulas: ##STR1## and pharmaceutically acceptable salts thereof which are useful for inducing immunosuppression and treating transplantation rejection, host vs. graft disease, autoimmune diseases, diseases of inflammation, solid tumors, fungal infections, adult T-cell leukemia/lymphomas and hyperproliferative vascular disorders.

US Patent:

55082858, Apr 16, 1996

Filed:

May 24, 1995

Appl. No.:

8/449168

Inventors:

Frances C. Nelson - Yardley PA
Guy A. Schiehser - Yardley PA

Assignee:

American Home Products Corporation - Madison NJ

International Classification:

A61K 31395
C07D49816

US Classification:

514291

Abstract:

A compound of the structure ##STR1## wherein R and R. sup. 1 are each, independently, ##STR2## or hydrogen; R. sup. 2 and R. sup. 3 are each, independently, alkyl, arylalkyl , or R. sup. 2 and R. sup. 3 may be taken together to form a cycloalkyl ring; R. sup. 4 is a heterocyclic N-oxide radical, which may be optionally substituted; R. sup. 5 is alkyl or arylalkyl; R. sup. 6 and R. sup. 7 are taken together to form a saturated N-alkyl-heterocyclic N-oxide, which may be optionally substituted; k=0-1, m=0-1; n=1-6; with the proviso that R and R. sup. 1 are not both hydrogen, which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.

US Patent:

54912318, Feb 13, 1996

Filed:

Nov 28, 1994

Appl. No.:

8/345972

Inventors:

Frances C. Nelson - Yardley PA
Guy A. Schiehser - Yardley PA

Assignee:

American Home Products Corporation - Madison NJ

International Classification:

A61K 31395
C02D49106

US Classification:

540456

Abstract:

A compound of the structure ##STR1## wherein R and R. sup. 1 are each, independently, ##STR2## or hydrogen; R. sup. 2 and R. sup. 3 are each, independently, alkyl, arylalkyl , or R. sup. 2 and R. sup. 3 may be taken together to form a cycloalkyl ring; R. sup. 4 is a heterocyclic N-oxide radical, which may be optionally substituted; R. sup. 5 is alkyl or arylalkyl; R. sup. 6 and R. sup. 7 are taken together to form a saturated N-alkyl-heterocyclic N-oxide, which may be optionally substituted; k=0-1, m=0-1; n=1-6; with the proviso that R and R. sup. 1 are not both hydrogen, which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.

US Patent:

53859090, Jan 31, 1995

Filed:

Nov 22, 1993

Appl. No.:

8/156208

Inventors:

Frances C. Nelson - Yardley PA
Guy A. Schiehser - Yardley PA

Assignee:

American Home Products Corporation - Madison NJ

International Classification:

A61K 31495
C07D48704

US Classification:

514291

Abstract:

A compound of the structure ##STR1## wherein R and R. sup. 1 are each, independently, ##STR2## or hydrogen, R. sup. 2 is a heterocyclic radical which may be optionally substituted; n=0-6; with the proviso that R and R. sup. 1 are both not hydrogen, or a pharmaceutically acceptable salt thereof which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.