Patents Represented by Attorney, Agent or Law Firm Arnold S. Milowsky
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Patent number: 6103708Abstract: 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: GrantFiled: May 10, 1999Date of Patent: August 15, 2000Assignee: American Home Products CorporationInventors: Paul J. Dollings, Robert E. McDevitt, Folake O. Adebayo
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Patent number: 6063815Abstract: 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: GrantFiled: May 10, 1999Date of Patent: May 16, 2000Assignee: American Home Products CorporationInventor: Paul J. Dollings
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Patent number: 6057316Abstract: 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: GrantFiled: May 10, 1999Date of Patent: May 2, 2000Assignee: American Home Products CorporationInventors: Jay E. Wrobel, Zenan Li
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Patent number: 6057340Abstract: 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: GrantFiled: February 3, 1999Date of Patent: May 2, 2000Assignee: American Home Products CorporationInventors: Michael G. Kelly, Lynne P. Greenblatt, Frances C. Nelson
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Patent number: 6015809Abstract: 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: GrantFiled: August 16, 1999Date of Patent: January 18, 2000Assignee: American Home Products CorporationInventors: Tianmin Zhu, Hyuk-Koo Lee
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Patent number: 6001867Abstract: 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: GrantFiled: May 10, 1999Date of Patent: December 14, 1999Assignee: American Home Products CorporationInventors: Jay E. Wrobel, Arlene J. Dietrich, Zenan Li
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Patent number: 6002008Abstract: 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: GrantFiled: March 27, 1998Date of Patent: December 14, 1999Assignee: American Cyanamid CompanyInventors: Allan Wissner, Bernard D. Johnson, Marvin F. Reich, Middleton B. Floyd, Jr., Douglas B. Kitchen, Hwei-Ru Tsou
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Patent number: 5998638Abstract: 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: GrantFiled: April 21, 1998Date of Patent: December 7, 1999Assignee: American Home Products CorporationInventors: Reinhold H. W. Bender, Mahdi B. Fawzi, Horace Fletcher, III, George O. Morton, Syed M. Shah, Xuejun Tang
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Patent number: 5989591Abstract: 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: GrantFiled: March 11, 1998Date of Patent: November 23, 1999Assignee: American Home Products CorporationInventor: Arwinder S. Nagi
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Patent number: 5985325Abstract: 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: GrantFiled: May 29, 1998Date of Patent: November 16, 1999Assignee: American Home Products CorporationInventor: Arwinder S. Nagi
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Patent number: 5955457Abstract: 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: GrantFiled: March 23, 1998Date of Patent: September 21, 1999Assignee: American Home Products CorporationInventors: Hyuk-Koo Lee, Tianmin Zhu
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Patent number: 5932585Abstract: 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: GrantFiled: December 16, 1997Date of Patent: August 3, 1999Assignee: American Cyanamid CompanyInventors: Joseph W. Epstein, Jeremy I. Levin, James J. Gibbons, Judy Lucas
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Patent number: 5929080Abstract: 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: GrantFiled: April 21, 1998Date of Patent: July 27, 1999Assignee: American Cyanamid CompanyInventor: Philip Frost
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Patent number: 5922730Abstract: 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: GrantFiled: June 24, 1998Date of Patent: July 13, 1999Assignee: American Home Products CorporationInventors: David Cheng Hu, Alexander Aleksey Greenfield, Thomas Joseph Caggiano, Craig Eugene Caufield
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Patent number: 5914327Abstract: 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: GrantFiled: November 6, 1997Date of Patent: June 22, 1999Assignee: American Cyanamid CompanyInventors: Michael P. Trova, Nan Zhang, Douglas B. Kitchen
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Patent number: 5908840Abstract: 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: GrantFiled: November 6, 1997Date of Patent: June 1, 1999Assignee: American Cyanamid CompanyInventors: Michael P. Trova, Nan Zhang
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Patent number: 5888543Abstract: 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: GrantFiled: July 2, 1997Date of Patent: March 30, 1999Assignee: American Home Products CorporationInventor: Michael J. Gast
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Patent number: 5869524Abstract: 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: GrantFiled: October 28, 1997Date of Patent: February 9, 1999Assignee: American Home Products CorporationInventor: Amedeo A. Failli
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Patent number: 5864040Abstract: 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: GrantFiled: December 23, 1996Date of Patent: January 26, 1999Assignee: American Home Products CorporationInventors: Reinhardt B. Baudy, Michel Bekhazi, Brian J. Bushell, deceased, by Judith Marion Bushell, executrix, Gloria Cheal
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Patent number: 5858405Abstract: 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: GrantFiled: July 2, 1997Date of Patent: January 12, 1999Assignee: American Home Products CorporationInventor: Michael J. Gast