Patents Represented by Attorney, Agent or Law Firm Arnold S. Milowsky
  • Patent number: 6103708
    Abstract: This invention provides compounds of Formula I having the structure: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, W, X, Y, and Z are as defined in the specification, or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.
    Type: Grant
    Filed: May 10, 1999
    Date of Patent: August 15, 2000
    Assignee: American Home Products Corporation
    Inventors: Paul J. Dollings, Robert E. McDevitt, Folake O. Adebayo
  • Patent number: 6063815
    Abstract: This invention provides compounds of Formula I having the structure ##STR1## wherein Y is ##STR2## R.sup.1 and R.sup.2 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, halogen, perfluoroalkyl of 1-6 carbon atoms, cycloalkyl of 3-8 carbon atoms, thienyl, furyl, phenyl or phenyl mono-, di- or tri-substituted with trifluoromethyl, chloro, methoxy, or trifluoromethoxy;R.sup.3 and R.sup.4 are each, independently, hydrogen, carboxyl, hydroxyl, hydoxyalkyl of 1-6 carbon atoms, hydroxyalkanoyl of 1-6 carbon atoms, aryloxycarbonyl of 7-13 carbon atoms, alkoxycarbonyl of 2-7 carbon atoms, perfluoroalkoxycarbonyl of 2-7 carbon atoms, alkyl of 1-6 carbon atoms, perfluoroalkyl of 1-6 carbon atoms, aminoalkyl of 1-6 carbon atoms, alkylamino of 1-6 carbon atoms, dialkylamino of 1-6 carbon atoms per alkyl group, tetrazolyl, mercapto, alkylsulfanyl of 1-6 carbon atoms, nitrile, nitro, amino, --NHSO.sub.2 CF.sub.
    Type: Grant
    Filed: May 10, 1999
    Date of Patent: May 16, 2000
    Assignee: American Home Products Corporation
    Inventor: Paul J. Dollings
  • Patent number: 6057340
    Abstract: This invention provides compounds of Formula 1 having the structure ##STR1## wherein: R.sub.1 is hydrogen, alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, benzyloxy, trifluoromethyl, chloro, bromo, or fluoro;a dashed line indicates an optional bond,X is NR.sub.4, or no atom;R.sub.2 is alkyl of 1-6 carbon atoms, cycloalkyl of 3-8 carbon atoms, cycloalkylalkyl wherein the cycloalkyl moiety is 3-8 carbon atoms and the alkyl moiety is 1-6 carbon atoms, aryl of 5-12 carbon atoms, or arylalkyl of 6-12 carbon atoms;R.sub.3 is aryl of 5-12 carbon atoms, arylalkyl of 6-12 carbon atoms, or heteroaryl of 5-12 atoms;R.sub.4 is hydrogen or alkyl of 1-6 carbon atoms;or a pharmaceutically acceptable salt thereof, which are useful in the treatment of psychosis (e.g. schizophrenia), anxiety, depression and related CNS disorders and other conditions such as the treatment of alcohol and drug withdrawal, sexual dysfunction and memory deficits associated with Alzheimer's disease and other dementias.
    Type: Grant
    Filed: February 3, 1999
    Date of Patent: May 2, 2000
    Assignee: American Home Products Corporation
    Inventors: Michael G. Kelly, Lynne P. Greenblatt, Frances C. Nelson
  • Patent number: 6057316
    Abstract: This invention provides compounds of Formula I having the structure ##STR1## wherein B and D are each, independently, hydrogen, halogen, --CN, alkyl of 1-6 carbon atoms, aryl, or aralkyl of 6-12 carbon atoms;R.sup.1 is hydrogen, alkyl of 1-6 carbon atoms, --CH(R.sup.2)W, --C(CH.sub.3).sub.2 CO.sub.2 R.sup.3, 5-thiazolidine-2,4-dione, --CH(R.sup.4)CH.sub.2 CO.sub.2 R.sup.3, --COR.sup.3, or --PO.sub.3 (R.sup.3).sub.2 ;R.sup.2 is hydrogen, alkyl of 1-6 carbon atoms, aralkyl of 6-12 carbon atoms, aryl, --CH.sub.2 (1H-imidazol-4-yl), --CH.sub.2 (3-1H-indolyl), --CH.sub.2 CH.sub.2 (1,3-dioxo-1,3-dihydro-isoindol-2-yl), --CH.sub.2 CH.sub.2 (1-oxo-1,3-dihydro-isoindol-2-yl), or --CH.sub.2 (3-pyridyl);W is --CO.sub.2 R.sup.3, --CONH.sub.2, --CONHOH, --CN, CONH(CH.sub.2).sub.2 CN, 5-tetrazole, or --PO.sub.3 (R.sup.3).sub.2 ;R.sup.3 is hydrogen, alkyl of 1-6 carbon atoms, or aryl;R.sup.
    Type: Grant
    Filed: May 10, 1999
    Date of Patent: May 2, 2000
    Assignee: American Home Products Corporation
    Inventors: Jay E. Wrobel, Zenan Li
  • Patent number: 6015809
    Abstract: A compound of the structure ##STR1## or a 31- and/or 42-ester or ether thereof, which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.
    Type: Grant
    Filed: August 16, 1999
    Date of Patent: January 18, 2000
    Assignee: American Home Products Corporation
    Inventors: Tianmin Zhu, Hyuk-Koo Lee
  • Patent number: 6002008
    Abstract: This invention provides compounds having the formula: ##STR1## wherein: X is cycloalkyl which may be optionally substituted; or is a pyridinyl, pyrimidinyl, or phenyl ring; wherein the pyridinyl, pyrimidinyl, or phenyl ring may be optionally substituted;n is 0-1;Y is --NH--, --O--, --S--, or --NR--;R is alkyl of 1-6 carbon atoms;R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are each, independently, hydrogen, halogen, alkyl, alkenyl, alkynyl, alkenyloxy, alkynyloxy, hydroxymethyl, halomethyl, alkanoyloxy, alkenoyloxy, alkynoyloxy, alkanoyloxymethyl, alkenoyloxymethyl, alkynoyloxymethyl, alkoxymethyl, alkoxy, alkylthio, alkylsulphinyl, alkylsulphonyl, alkylsulfonamido, alkenylsulfonamido, alkynylsulfonamido, hydroxy, trifluoromethyl, cyano, nitro, carboxy, carboalkoxy, carboalkyl, phenoxy, phenyl, thiophenoxy, benzyl, amino, hydroxyamino, alkoxyamino, alkylamino, dialkylamino, aminoalkyl, N-alkylaminoalkyl, N,N-dialkylaminoalkyl, phenylamino, benzylamino, ##STR2## R.sub.
    Type: Grant
    Filed: March 27, 1998
    Date of Patent: December 14, 1999
    Assignee: American Cyanamid Company
    Inventors: Allan Wissner, Bernard D. Johnson, Marvin F. Reich, Middleton B. Floyd, Jr., Douglas B. Kitchen, Hwei-Ru Tsou
  • Patent number: 6001867
    Abstract: This invention provides compounds of Formula I having the structure ##STR1## wherein: B and D are each, independently, hydrogen, halogen, --CN, alkyl of 1-6 carbon atoms, aryl, aralkyl of 6-12 carbon atoms;X is H, or halogen;R.sup.1 is hydrogen, alkyl of 1-6 carbon atoms, --CH(R.sup.2)W, --C(CH.sub.3).sub.2 CO.sub.2 R.sup.3, 5-thiazolidine-2,4-dione, --CH(R.sup.4)CH.sub.2 CO.sub.2 R.sup.3, --COR.sup.3, or --PO.sub.3 (R.sup.3).sub.2 ;R.sup.2 is hydrogen, alkyl of 1-6 carbon atoms, aralkyl of 6-12 carbon atoms, aryl, --CH.sub.2 (1H-imidazol-4-yl), --CH.sub.2 (3-1H-indolyl), --CH.sub.2 CH.sub.2 (1,3-dioxo-1,3-dihydro-isoindol-2-yl), --CH.sub.2 CH.sub.2 (1-oxo-1,3-dihydro-isoindol-2-yl), or --CH.sub.2 (3-pyridyl);W is --CO.sub.2 R.sup.3, --CONH.sub.2, --CONHOH, --CN, --CONH(CH.sub.2).sub.2 CN, 5-tetrazole, or --PO.sub.3 (R.sup.3).sub.2 ;R.sup.3 is hydrogen, alkyl of 1-6 carbon atoms, or aryl;R.sup.
    Type: Grant
    Filed: May 10, 1999
    Date of Patent: December 14, 1999
    Assignee: American Home Products Corporation
    Inventors: Jay E. Wrobel, Arlene J. Dietrich, Zenan Li
  • Patent number: 5998638
    Abstract: This invention provides a pharmaceutically acceptable salt of 5.alpha.-pregn-16-3.beta.-ol-20-one 3-sulfate ester, which is useful as a progestational agent.
    Type: Grant
    Filed: April 21, 1998
    Date of Patent: December 7, 1999
    Assignee: American Home Products Corporation
    Inventors: Reinhold H. W. Bender, Mahdi B. Fawzi, Horace Fletcher, III, George O. Morton, Syed M. Shah, Xuejun Tang
  • Patent number: 5989591
    Abstract: This invention provides rapamycin solid dosage unit which comprises a core and a sugar overcoat, said sugar overcoat comprising rapamycin, one or more surface modifying agents, one or more sugars, and optionally one or more binders.
    Type: Grant
    Filed: March 11, 1998
    Date of Patent: November 23, 1999
    Assignee: American Home Products Corporation
    Inventor: Arwinder S. Nagi
  • Patent number: 5985325
    Abstract: This invention provides rapamycin solid dosage unit which comprises a core and a sugar overcoat, said sugar overcoat comprising rapamycin, one or more sugars, and one or more binders.
    Type: Grant
    Filed: May 29, 1998
    Date of Patent: November 16, 1999
    Assignee: American Home Products Corporation
    Inventor: Arwinder S. Nagi
  • Patent number: 5955457
    Abstract: A compound of the structure ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen or --COCH.sub.2 --S--CH.sub.2 CH.sub.2 --O--CH.sub.2 --(CH.sub.2 OCH.sub.2).sub.n --CH.sub.2 --O--CH.sub.2 CH.sub.2 --OCH.sub.3 ; and n=8-450; with the proviso that R.sup.1 and R.sup.2 are not both hydrogen, which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.
    Type: Grant
    Filed: March 23, 1998
    Date of Patent: September 21, 1999
    Assignee: American Home Products Corporation
    Inventors: Hyuk-Koo Lee, Tianmin Zhu
  • Patent number: 5932585
    Abstract: The invention is a method of treating or inhibiting neutropenia, or accelerating neutrophil recovery in a mammal in need thereof, which comprises administering to said mammal an effective amount of a compound having the formula: ##STR1## wherein R.sub.1 and R.sub.2 are each, independently selected from the group consisting of hydrogen, alkyl of 1-6 carbon atoms, optionally substituted benzoyl, ##STR2## or R.sub.1 and R.sub.2 are methylene groups which are taken together to form a 4-7 membered saturated heterocyclic ring;R is hydroxy, 4-morpholinyl, 1H-imidazol-1 -yl, --CH(alkoxy of 1-6 carbon atoms).sub.2, .alpha.-hydroxybenzyl, or optionally substituted phenyl;R.sub.3 is hydrogen or alkyl; R.sub.4 is hydrogen, halogen, alkyl, alkoxy, or trifluoromethyl; R.sub.5 is hydrogen or alkyl; and n=1-3, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: December 16, 1997
    Date of Patent: August 3, 1999
    Assignee: American Cyanamid Company
    Inventors: Joseph W. Epstein, Jeremy I. Levin, James J. Gibbons, Judy Lucas
  • Patent number: 5929080
    Abstract: This invention provides a method of treating or inhibiting polycystic kidney disease in a mammal in need thereof which comprises administering to said mammal a compound having the formula ##STR1## wherein: X is phenyl which is optionally substituted;R and R.sub.1 are each, independently, hydrogen, halogen, alkyl, alkoxy, hydroxy, or trifluoromethyl;R.sub.2 is hydrogen, alkyl, alkoxy, hydroxy, trifluoromethyl;Y is a radical selected from the group consisting of ##STR2## R.sub.3 is independently hydrogen, alkyl, carboxy, carboalkoxy, phenyl, or carboalkyl; n=2-4;or a pharmaceutically acceptable salt thereof, with the proviso that each R.sub.3 of Y may be the same or different.
    Type: Grant
    Filed: April 21, 1998
    Date of Patent: July 27, 1999
    Assignee: American Cyanamid Company
    Inventor: Philip Frost
  • Patent number: 5922730
    Abstract: This invention relates to compounds which possess immunosuppressive and/or anti tumor and/or antinflammatory activity in vivo and/or inhibit thymocyte proliferation in vitro. These compounds are therefore useful in the treaiment of transplantation rejection, autoimmune diseases such as lupus, rheumatoid ardiritis, diabetes mellitus, multiple sclerosis and in the treatment of Candida albicans infections and also in treatment of diseases of inflammation. These compounds are represented by the formula below ##STR1## wherein W and Y are OR.sup.1 and X and Z together form a bond or W and X are OR.sup.2 and Y and Z together form a bond, wherein:R.sup.1 is selected from --(CH.sub.2).sub.n --Ar with a proviso that Ar is not phenyl,--(CH.sub.2 CH.sub.2 O).sub.n CH.sub.3 with a proviso that n is greater than one,--CH.sub.2 CH.sub.2 CH.sub.2 O(CH.sub.2 CH.sub.2 O).sub.m --CH.sub.3,--(CH.sub.2).sub.n --CH.sub.2 CH(OR.sup.3)CH.sub.2 OR.sup.4 where R.sup.3 and R.sup.4 are H, C.sub.1 -C.sub.10 alkyl, or R.sup.3 and R.sup.
    Type: Grant
    Filed: June 24, 1998
    Date of Patent: July 13, 1999
    Assignee: American Home Products Corporation
    Inventors: David Cheng Hu, Alexander Aleksey Greenfield, Thomas Joseph Caggiano, Craig Eugene Caufield
  • Patent number: 5914327
    Abstract: This invention provides a compound having the formula: ##STR1## wherein: (A) n=2-4;(B) R.sub.1 and R.sub.2 are the same or different and selected from the group consisting of H, (C.sub.1 -C.sub.3)alkyl, --CH.sub.2 CH.sub.2 OH, --CH.sub.2 CH.sub.2 NH.sub.2, and --CH.sub.2 CH.sub.2 N(CH.sub.3).sub.2 or R.sub.1 and R.sub.2 are alkyl moieties which may taken together to form a 4- to 7-membered ring;(C) R.sub.3 is selected from H, --CH.sub.3, --CH.sub.2 CH.sub.3, --CH.sub.2 CH.sub.2 NH.sub.2 ;(D) X is located at the 2-, or 3-position and is selected from the group consisting of 2-naphthyl, 1-naphthyl, 1-phenanthrenyl, 2-phenanthrenyl, 3-phenanthrenyl, 4-phenanthrenyl, 9-phenanthrenyl, phenyl, and mono- or polysubstituted phenyl wherein the substituents are selected from the group consisting of --OR.sub.4, --NR.sub.5 R.sub.6, (C.sub.1 -C.sub.3) alkyl, --CF.sub.3, F, Cl, Br, I, --NO.sub.2, --CN, --SO.sub.3 H, --SO.sub.2 NR.sub.5 R.sub.6, --CO.sub.2 H, --CO.sub.2 R.sub.4, and phenyl;R.sub.4 is H or (C.sub.1 -C.sub.
    Type: Grant
    Filed: November 6, 1997
    Date of Patent: June 22, 1999
    Assignee: American Cyanamid Company
    Inventors: Michael P. Trova, Nan Zhang, Douglas B. Kitchen
  • Patent number: 5908840
    Abstract: This invention provides a compound having the formula: ##STR1## wherein: (A) n=2-4;(B) R.sub.1 and R.sub.2 are the same or different and selected from the group consisting of H, (C.sub.1 -C.sub.3) alkyl, --CH.sub.2 CH.sub.2 OH, --CH.sub.2 CH.sub.2 NH.sub.2, and --CH.sub.2 CH.sub.2 N(CH.sub.3).sub.2 or R.sub.1 and R.sub.2 are alkyl moieties which are taken together to form a 4- to 7- membered ring;(C) R.sub.3 is selected from the group consisting of H, --CH.sub.3, --CH.sub.2 CH.sub.3, and --CH.sub.2 CH.sub.2 NH.sub.2 ;(D) Y is a heterocyclic radical having 5-14 atoms, located at the 2- or 3- position of the pyridoquinazolinone nucleus, in which 1-3 of the heterocyclic ring atoms are independently nitrogen, oxygen, or sulfur; wherein Y may be optionally mono-, di-, or tri- substituted with --OR.sub.4, --NR.sub.5 R.sub.6, --CO.sub.2 H, --CO.sub.2 R.sub.4, or phenyl;R.sub.4 is H or (C.sub.1 -C.sub. 4) straight-chain alkyl;R.sub.5 and R.sub.
    Type: Grant
    Filed: November 6, 1997
    Date of Patent: June 1, 1999
    Assignee: American Cyanamid Company
    Inventors: Michael P. Trova, Nan Zhang
  • Patent number: 5888543
    Abstract: This invention provides a method of contraception which comprises administering to a female of child bearing age for 23-25 consecutive days, a first phase combination of a progestin at a daily dosage of 40-500 .mu.g trimegestone, 250 .mu.g-4 mg dienogest, or 250 .mu.g-4 mg drospirenone, and an estrogen at a daily dosage equivalent in estrogenic activity to 10-20 .mu.g ethinyl estradiol for 9-13 days beginning on day 1 of the menstrual cycle, wherein the same dosage of the progestin and estrogen combination is administered in each of the 9-13 days, and a second phase combination of a progestin at a daily dosage of 40-500 .mu.g trimegestone, 250 .mu.g-4 mg dienogest, or 250 .mu.g-4 mg drospirenone, and an estrogen at a daily dosage equivalent in estrogenic activity to 10-20 .mu.
    Type: Grant
    Filed: July 2, 1997
    Date of Patent: March 30, 1999
    Assignee: American Home Products Corporation
    Inventor: Michael J. Gast
  • Patent number: 5869524
    Abstract: This invention provides compounds of formula 1 having the structure ##STR1## wherein: R.sup.1 is hydrogen, halogen, alkyl, alkoxy, fluoroalkoxy, trifluoromethyl, alkylthio, or SCF.sub.3R.sup.2 and R.sup.3 are each independently, hydrogen or alkyl, or R.sup.2 and R.sup.3 may be taken together to form a saturated cycloalkyl ring; andR.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are each independently, hydrogen, alkyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, halogen, fluoroalkoxy, CF.sub.3, or SCF.sub.3 which are useful in the treatment of arthritic disorders, colorectal cancer, and Alzheimer's disease.
    Type: Grant
    Filed: October 28, 1997
    Date of Patent: February 9, 1999
    Assignee: American Home Products Corporation
    Inventor: Amedeo A. Failli
  • Patent number: 5864040
    Abstract: This invention provides a process for the preparation of a compound of formula I ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen, alkyl, alkoxy, trifluoromethyl, trifluoromethoxy, methanesulfonylamino, acetylamino, halo, cyano, nitro, or when taken together R.sup.1 and R.sup.2 represent a methylenedioxy or ethylenedioxy moiety;or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: December 23, 1996
    Date of Patent: January 26, 1999
    Assignee: American Home Products Corporation
    Inventors: Reinhardt B. Baudy, Michel Bekhazi, Brian J. Bushell, deceased, by Judith Marion Bushell, executrix, Gloria Cheal
  • Patent number: 5858405
    Abstract: This invention provides a bridged triphasic combination progestin/estrogen oral contraceptive regimen comprising the administration of a contraceptive progestin/estrogen combination for 23-25 days consecutive days beginning on the first day of menses, followed by the administration of an estrogen for 3-5 days following the administration of the estrogen/progestin combination, so that the total period of administration is 28 days per 28 day cycle. Particularly preferred progestins of this invention are trimegestone, dienogest, and drospirenone.
    Type: Grant
    Filed: July 2, 1997
    Date of Patent: January 12, 1999
    Assignee: American Home Products Corporation
    Inventor: Michael J. Gast