Patents Represented by Attorney, Agent or Law Firm Arnold S. Milowsky
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Patent number: 5830911Abstract: This invention provides compounds of formula I having the structure ##STR1## wherein R is (CH.sub.2).sub.n COOR.sup.4 ;R.sup.1 is hydrogen, alkyl, alkenyl, alkynyl, alkylcycloalkyl, and alkoxyalkyl;R.sup.4 is hydrogen or alkyl;R.sup.5, R.sup.6, R.sup.7, and R.sup.8 are each, independently, hydrogen, halogen, alkyl, alkenyl, alkynyl, alkoxy, arylalkoxy, fluoroalkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, cyano, nitro, --SCF.sub.3, --COR.sup.3, alkanoyloxy, hydroxy, trifluoromethyl, amino, alkylamino, dialkylamino, alkylamido, or alkylsulfonamido; wherein at least one of R.sup.5, R.sup.6, R.sup.7, or R.sup.8 is cyano;R.sup.3 is alkyl, hydroxy, alkoxy, amino, alkylamino;X is --O-- or --C--; andn=1-4or a pharmaceutically acceptable salt thereof, which are useful in the treatment of arthritic disorders, colorectal cancer, and Alzheimer's disease.Type: GrantFiled: August 5, 1997Date of Patent: November 3, 1998Assignee: American Home Products CorporationInventors: Amedeo A. Failli, Robert J. Steffan, Anthony F. Kreft, Thomas J. Caggiano, Craig E. Caufield
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Patent number: 5824699Abstract: This invention provides compounds of formula I having the structure ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are, each, independently, hydrogen, alkyl, alkenyl, alkynyl, alkoxy, aralkoxy, trifluroalkoxy, alkanoyloxy, hydroxy, halo, trifluoromethyl, cyano, amino, mono- or di-alkylamino, alkanamido, or alkanesulfonamido;R.sub.5 is hydrogen, alkyl, alkenyl, alkoxyalkyl or alkylcycloalkyl;R.sub.6 is hydrogen, alkyl or alkenyl;X is oxygen or carbon;A is oxygen or NZ;Z is hydroxyl, alkoxy, aryloxy, carboxyalkyloxy of 2-7 carbon atoms, arylamino, or alkylsulfonyamino of 1-6 carbon atoms;or a pharmaceutically acceptable salt thereof, which are useful in the treatment of arthritic disorders, colorectal cancer, and Alzheimer's disease.Type: GrantFiled: March 16, 1998Date of Patent: October 20, 1998Assignee: American Home Products CorporationInventors: Anthony F. Kreft, Craig E. Caufield, Amedeo A. Failli, Thomas J. Caggiano, Alexander A. Greenfield, Dennis M. Kubrak
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Patent number: 5817064Abstract: A cartridge syringe with a slideable protective sheath to prevent accidental needle sticks following administration of a an injection is described. The device comprises a syringe cartridge, comprising a constricted distal end region, a piston movably disposed within the barrel, a hub having an axial bore mounted to the constricted distal end region of the barrel, and a hollow needle, the proximal end of the hollow needle projecting through the axial bore of the hub and the distal end of the needle having a pointed tip; and a protective sheath having an inner diameter greater than the external diameter of the syringe cartridge, such that the protective sheath is slideably movable substantially coaxially along the external surface of the cartridge barrel from a first position in which the tip of the needle extends past both ends of the protective sheath, to a second position in which the distal end of the sheath extends past the tip of the needle.Type: GrantFiled: October 15, 1996Date of Patent: October 6, 1998Assignee: American Home Products CorporationInventors: Anthony O. DeMarco, Stephen W. Goodsir
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Patent number: 5780462Abstract: A compound of the structure ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen orCOCH.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: December 11, 1996Date of Patent: July 14, 1998Assignee: American Home Products CorporationInventors: Hyuk-Koo Lee, Tianmin Zhu
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Patent number: 5776943Abstract: This invention provides metabolites of rapamycin, the first of which is 41-O-desmethyl rapamycin, having a deprotonated molecular ion detected at a mass to charge ratio of 899, and a characteristic desorption chemical ionization mass spectroscopic fragmentation pattern comprising ions detected at a mass to charge ratio of 591, 569, 559, 543, 529, 421, and 308. A second compound of this invention is a hydroxylated metabolite of rapamycin having a deprotonated molecular ion detected at a mass to charge ratio of 928, and a characteristic direct chemical ionization mass spectroscopic fragmentation pattern comprising ions detected at a mass to charge ratio of 607, 571, 545, 513, 322, 290, and 241 amu. The compounds of this invention, by virtue of their immunosuppressive activity are useful in treating transplantation rejection, host vs.Type: GrantFiled: May 14, 1991Date of Patent: July 7, 1998Assignee: American Home Products CorporationInventors: Uwe Christians, Karl F. Sewing, Martin Sattler
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Patent number: 5776967Abstract: This invention provides compounds of formula I having the structure ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are, each, independently, hydrogen, alkyl, alkenyl, alkynyl, alkoxy, aralkoxy, trifluroalkoxy, alkanoyloxy, hydroxy, halo, trifluoromethyl, cyano, amino, mono- or di-alkylamino, alkanamido, or alkanesulfonamido;R.sub.5 is hydrogen, alkyl, alkenyl, alkoxyalkyl or alkylcycloalkyl;R.sub.6 is hydrogen, alkyl or alkenyl;X is oxygen or carbon;A is oxygen or NZ;Z is hydroxyl, alkoxy, aryloxy, carboxyalkyloxy of 2-7 carbon atoms, arylamino, or alkylsulfonyamino of 1-6 carbon atoms;or a pharmaceutically acceptable salt thereof, which are useful in the treatment of arthritic disorders, colorectal cancer, and Alzheimer's disease.Type: GrantFiled: July 7, 1997Date of Patent: July 7, 1998Assignee: American Home Products CorporationInventors: Anthony F. Kreft, Craig E. Caufield, Amedeo A. Failli, Thomas J. Caggiano, Alexander A. Greenfield, Dennis M. Kubrak
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Patent number: 5760041Abstract: This invention provides 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 which are useful as antineoplastic agents.Type: GrantFiled: January 21, 1997Date of Patent: June 2, 1998Assignee: American Cyanamid CompanyInventors: Allan Wissner, Bernard D. Johnson, Middleton B. Floyd, Jr., Douglas B. Kitchen
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Patent number: 5750522Abstract: This invention provides compounds having the formula ##STR1## wherein R is azacycle or azabicycle;R.sub.1 is alkyl;R.sub.2 and R.sub.3 are each, independently, hydrogen, alkyl, alkoxy, or thioalkyl;n is 0-5;or a pharmaceutically acceptable salt thereof, which are useful in treating symptoms of cholinergic insufficiency involving cognitive disorders.Type: GrantFiled: July 12, 1996Date of Patent: May 12, 1998Assignee: American Home Products CorporationInventors: Annmarie Louise Sabb, William A. Kinney
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Patent number: 5747480Abstract: This invention provides a method of contraception which comprises administering to a female of child bearing age for 28 consecutive days,a first phase combination of a progestin at a daily dosage equivalent in progestational activity to 40-125 .mu.g levonorgestrel and an estrogen at a daily dosage equivalent in estrogenic activity to 10-20 .mu.g ethinyl estradiol for 3-8 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 3-8 days,a second phase combination of a progestin at a daily dosage equivalent in progestational activity to 40-125 .mu.g levonorgestrel and an estrogen at a daily dosage equivalent in estrogenic activity to 10-20 .mu.Type: GrantFiled: April 17, 1997Date of Patent: May 5, 1998Assignee: American Home Products CorporationInventor: Michael J. Gast
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Patent number: 5728727Abstract: A compound of Formula I, which is named {5R*-?6R*, 7S*, 8R*, 9R*, 12S*, 16S*, 18S*, 19S*, (13E)!} 4, 7, 19-trihydroxy-2, 6, 8, 12, 12, 14, 16, 18-heptamethyl-6, 7, 8, 9, 10, 11, 12, 15, 16, 17, 18, 19-dodecahydro-1, 19:5, 9-diepoxybenzocyclooctadecen-3 (5H)-one, and which is useful in inhibiting bone resorption, and treating and inhibiting osteoporosis.Type: GrantFiled: October 3, 1996Date of Patent: March 17, 1998Assignee: American Home Products CorporationInventors: Michael H. Su, Margaret I. Hosken, Brian J. Hotovec, Terra L. Johnston
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Patent number: 5719153Abstract: This invention provides compounds having the structure ##STR1## wherein m=0-1; andn=0-1 or a pharmaceutically acceptable salt thereof when m and n=0, that are useful as neuroprotective agents.Type: GrantFiled: August 6, 1996Date of Patent: February 17, 1998Assignee: American Home Products CorporationInventors: Reinhardt B. Baudy, Theodore S. Sulkowski
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Patent number: 5677295Abstract: A compound of the structure ##STR1## wherein X--Y is C.dbd.NOR.sup.1 or CHNHOR.sup.2 ; R.sup.1 and R.sup.2 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, cycloalkyl, alkyloxy, alkoxyalkyl, cycloalkylaminoalkyl, cyanoalkyl, fluoroalkyl, trifluoromethylalkyl, trifluoromethyl, ArO--, --(CH.sub.2).sub.m Ar, or --COR.sup.3 ;R.sup.3 is alkyl of 1-6 carbon atoms, --NH.sub.2, --NHR.sup.4, --NR.sup.4 R.sup.5, or --OR.sup.4 ;R.sup.4 and R.sup.5 are each, independently, alkyl, Ar or if both are present can be taken together to form a 4-7 membered ring;Ar is an aryl or heteroaryl radical which may be optionally substituted; and m=0-6; or a pharmaceutically acceptable salt thereof, which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.Type: GrantFiled: May 30, 1996Date of Patent: October 14, 1997Inventors: Amedeo A. Failli, Guy A. Schiehser, Oleg I. Bleyman
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Patent number: 5665728Abstract: This invention provides a method of preventing or treating hyperproliferative vascular disease in a mammal by administering an antiproliferative effective amount of rapamycin alone or in combination with mycophenolic acid.Type: GrantFiled: May 26, 1995Date of Patent: September 9, 1997Assignee: American Home Products CorporationInventors: Randall Ellis Morris, Clare Robert Gregory
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Patent number: 5658945Abstract: The invention relates to novel ureas and urethanes of Formula I: ##STR1## which stimulate cytokine production and may be used to accelerate recovery from neutropenia accompanying radio- or chemotherapy, bone marrow transplantation, or infections. Compounds in the invention or pharmaceutical compositions employing these compounds may be useful in the treatment of cancer, AIDS, aplastic anemia, myelodysplastic syndrome, and infectious diseases, and in the enhancement of immune response.Type: GrantFiled: May 25, 1995Date of Patent: August 19, 1997Assignee: American Cyanamid CompanyInventors: Semiramis Ayral-Kaloustian, Steven R. Schow, Mila T. Du, James J. Gibbons, Jr.
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Patent number: 5654436Abstract: Disclosed herein are compounds of the formula: ##STR1## where R.sub.1 is alkyl, trifluoromethyl or pyridinyl;R.sub.2 is H, alkyl or substituted arylalkyl, in which the substituents are one or two halogens, carboxyl or alkoxycarbonyl groups;R.sub.3 and R.sub.4 are H, alkyl, halogen or nitro;or a pharmaceutically acceptable salt thereof, which are useful as inhibitors of smooth muscle cell proliferation.Type: GrantFiled: June 7, 1995Date of Patent: August 5, 1997Assignee: American Home Products CorporationInventors: Hassan M. Elokdah, Sie-Yearl Chai, Theodore S. Sulkowski
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Patent number: 5646160Abstract: This invention provides a method of preventing or treating hyperproliferative vascular disease in a mammal by administering an antiproliferative effective amount of rapamycin alone or in combination with mycophenolic acid.Type: GrantFiled: May 26, 1995Date of Patent: July 8, 1997Assignee: American Home Products CorporationInventors: Randall Ellis Morris, Clare Robert Gregory
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Patent number: 5639887Abstract: Compounds of the general formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are herein described, A is a straight or branched (C.sub.2 -C.sub.12)alkyl or a phenyl moiety and B is a moiety of the formula: ##STR2## The compounds are effective in potentiating the activity of chemotherapeutic anti-cancer agents by increasing the sensitivity of multi-drug resistant cells to such chemotherapeutic agents.Type: GrantFiled: May 25, 1995Date of Patent: June 17, 1997Assignee: American Cyanamid CompanyInventors: Dennis Powell, Rolf Paul, William A. Hallett, Dan M. Berger, Minu D. Dutia
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Patent number: 5637590Abstract: A compound of the structure ##STR1## wherein R and R.sup.1 are each, independently, hydrogen, or ##STR2## R.sup.2 and R.sup.3 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, --CO.sub.2 R.sup.5, --COR.sup.5, --CN, --NO.sub.2, --SO.sub.2 R.sup.5, --SO.sub.3 R.sup.5, --OR.sup.5, --SR.sup.5, or Ar;R.sup.4 is hydrogen, alkyl, alkenyl, alkynyl, --CF.sub.3, --NR.sup.5 R.sup.6, --CO.sub.2 R.sup.5, --COR.sup.5, CONR.sup.5 R.sup.6, --NO.sub.2, halogen, --OR.sup.5, --SR.sup.5, --CN, --SO.sub.2 R.sup.5, --SO.sub.3 R.sup.5, --SO.sub.2 NR.sup.5 R.sup.6, or Ar;R.sup.5 and R.sup.6 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, or Ar;Ar is phenyl, naphthyl, or hetaryl, wherein the foregoing may be optionally substituted;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.Type: GrantFiled: May 24, 1995Date of Patent: June 10, 1997Assignee: American Home Products CorporationInventors: Jerauld S. Skotnicki, Yvette L. Palmer
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Patent number: 5633280Abstract: The invention relates to novel ureas and urethanes of Formula I: ##STR1## which stimulate cytokine production and may be used to accelerate recovery from neutropenia accompanying radio- or chemotherapy, bone marrow transplantation, or infections. Compounds in the invention or pharmaceutical compositions employing these compounds may be useful in the treatment of cancer, AIDS, aplastic anemia, myelodysplastic syndrome, and infectious diseases, and in the enhancement of immune response.Type: GrantFiled: May 25, 1995Date of Patent: May 27, 1997Assignee: American Cyanamid CompanyInventors: Semiramis Ayral-Kaloustian, Steven R. Schow, Mila T. Du, James J. Gibbons, Jr.
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Patent number: 5616612Abstract: The invention relates to novel ureas and urethanes of Formula I: ##STR1## which stimulate cytokine production and may be used to accelerate recovery from neutropenia accompanying radio- or chemotherapy, bone marrow transplantation, or infections. Compounds in the invention or pharmaceutical compositions employing these compounds may be useful in the treatment of cancer, AIDS, aplastic anemia, myelodysplastic syndrome, and infectious diseases, and in the enhancement of immune response.Type: GrantFiled: May 25, 1995Date of Patent: April 1, 1997Assignee: American Cyanamid CompanyInventors: Semiramis Ayral-Kaloustian, Steven R. Schow, Mila T. Du, James J. Gibbons, Jr.