Leukemia Patents (Class 514/908)
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Patent number: 4931553Abstract: Platinum(amine) complexes, when covalently linked to a water-soluble, biodegradable or biostable polymer, exhibit high antitumor activity at low dosages of platinum against L1210 and solid tumors. The complexes are platinum square planar complexes and octahedral structures of the formulae ##STR1## wherein A.sub.2 represents either 2 ammonia ligands, 2 monodentate amine ligands or a single bidentate amine ligand; P is either a biodegradable or a biostable but biocompatible polymer having pendent anionic groups which form covalent linkages with Pt; o is a positive integer and X is an anionic ligand.Type: GrantFiled: May 11, 1988Date of Patent: June 5, 1990Inventors: Devinder S. Gill, Peter J. Andrulis, Jr.
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Patent number: 4927571Abstract: An doxorubicin/lyposome composition which can be reconstituted from a lyophilized form to an injectable liposome suspension having selected liposome sizes in the size range between 0.1 and 0.5 microns, and between about 85-95% liposome-entrapped doxorubicin. The composition is prepared by reconstituting a lyophilized doxorubicin/liposome composition to a liposome concentrate, then diluting the concentrate for perenteral.Type: GrantFiled: May 18, 1987Date of Patent: May 22, 1990Assignee: Liposome Technology, Inc.Inventors: Anthony H. Huang, Satya Krishnan
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Patent number: 4920126Abstract: N-(2-Fluorophenyl)-1,2,3,4-tetrahydro-6-hydroxy-2,4-dioxo-5-pyrimidinecarbo xamide, useful for regressing or inhibiting the growth of leukemia and tumors in mammals. The compound has the formula: ##STR1## wherein R.sub.1 and R.sub.2 are selected from hydrogen or a cyclic or acyclic group which forms pyrimidine nucleosides or pseudo nucleosides, and the pharmacologically acceptable acid addition salts thereof.Type: GrantFiled: May 10, 1988Date of Patent: April 24, 1990Assignee: Uniroyal Chemical Ltd/Uniroyal Chemical LteeInventor: Arthur D. Brewer
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Patent number: 4918101Abstract: The present invention relates to antitumor compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monomethyl or monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 29 carbon atoms in total); ethers, esters thereof; acid addition salts thereof; wherein Ar is a fused tetracyclic aromatic ring system comprised of 5-membered and 6-membered rings and contains at least one heteroatom and 3 aromatic rings and a total of no more than 18 ring atoms, or a substituted derivative thereof; the heteroatom is preferably oxygen, sulfur or nitrogen; when it is nitrogen this is substituted by hydrogen, methyl or ethyl;R.sup.1 contains not more than eight carbon atoms and is a group ##STR1## wherein m is O or 1;R.sup.5 is hydrogen;R.sup.6 and R.sup.7 are the same or different and each is hydrogen or C.sub.1-5 alkyl optionally substituted by hydroxy;R.sup.8 and R.sup.9 are the same or different and each is hydrogen or C.sub.Type: GrantFiled: August 19, 1988Date of Patent: April 17, 1990Assignee: Burroughs Wellcome Co.Inventor: Kenneth W. Bair
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Patent number: 4910218Abstract: The present invention relates to anti tumor compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monomethyl or monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 29 carbon atoms in total); ethers, esters thereof; acid addition salts thereof; wherein Ar is a fused tetracyclic aromatic ring system comprised of 5-membered and 6-membered rings and contains at least one heteroatom and 3 aromatic rings and a total of no more than 18 ring atoms, or a substituted derivative thereof; the heteroatom is preferably oxygen, sulfur or nitrogen; when it is nitrogen this is substituted by hydrogen, methyl or ethyl; R.sup.1 contains not more than eight carbon atoms and is a group ##STR1## wherein m is 0 or 1;R.sup.5 is hydrogen;R.sup.6 and R.sup.7 are the same or different and each is hydrogen or C.sub.1-5 alkyl optionally substituted by hydroxy;R.sup.8 and R.sup.9 are the same or different and each is hydrogen or C.sub.Type: GrantFiled: May 12, 1987Date of Patent: March 20, 1990Assignee: Burroughs Wellcome Co.Inventor: Kenneth W. Bair
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Patent number: 4904768Abstract: Phosphate derivatives of 4'-demethylepipodophyllotoxin glucosides are novel antitumor agents and the salts thereof offer the pharmaceutical advantage of high water solubility.Type: GrantFiled: May 27, 1988Date of Patent: February 27, 1990Assignee: Bristol-Myers CompanyInventors: Mark G. Saulnier, Peter D. Senter, John F. Kadow
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Patent number: 4894451Abstract: The disclosure describes unsymmetrical 1,4-bis-(aminoalkylamino)-anthracene-9,10-diones useful in the treatment of neoplasms. Also described is a process of preparing same starting from 1,4-dimethoxyanthracene-9,10-dione which is reacted with an aminoalkylamine. The reaction product is treated with a dialkylaminoethylamine or a N-heteroethylamine to give the unsymmetrical compound.Type: GrantFiled: July 19, 1988Date of Patent: January 16, 1990Assignee: The University of VermontInventors: A. Paul Krapcho, Miles P. Hacker, John J. Landi, Jr., J. J. McCormack, Kenneth J. Shaw
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Patent number: 4892963Abstract: Compounds of the following formula have pharmaceutical properties: ##STR1## in which X is R.sup.1 (HO)C.dbd.C(CN)--, R.sup.1 (CO)--CH(CN)-- or ##STR2## R.sup.1 and R.sup.2 are each hydrogen or C.sub.1-6 alkyl, R.sup.3, R.sup.4 and R.sup.5 are each hydrogen, hydroxy, halogen, nitro, cyano, carboxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, halo-substituted C.sub.1-4 alkyl, halo-substituted C.sub.1-4 alkoxy, halo-substituted C.sub.1-4 alkylthio, C.sub.2-5 alkoxycarbonyl, optionally substituted phenyl, optionally substituted phenoxy, R'R"N- where R' and R" are each hydrogen or C.sub.1-4 alkyl R'"CONH-- where R'" is C.sub.1-4 alkyl, R.sup.6, R.sup.7 and R.sup.8 are each C.sub.1-6 alkyl, halo-substituted C.sub.1-6 alkyl or optionally substituted phenyl, or R.sup.6 and R.sup.7, together with the carbon atom to which they are attached, form a cycloalkyl group containing 3 to 7 carbon atoms, or R.sup.6, R.sup.7 and R.sup.Type: GrantFiled: August 7, 1987Date of Patent: January 9, 1990Assignee: Lilly Industries LimitedInventors: Peter T. Gallagher, Terence A. Hicks, Graham W. Mullier
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Patent number: 4888419Abstract: This invention relates to novel 3'-demethoxy epipodophyllotoxin glucosides, their use as anti-tumor agents, and pharmaceutical compositions thereof.Type: GrantFiled: August 31, 1987Date of Patent: December 19, 1989Assignee: Bristol-Myers CompanyInventors: Mark G. Saulnier, Dolatrai M. Vyas
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Patent number: 4877777Abstract: A new class of soluble phosphorylated glucans is described as well as the process for making the same. According to a preferred embodiment, the soluble phosphorylated glucan is derived from the yeast Saccharomyces cerevisiae. The soluble phosphorylated glucans are useful for prophylactic and therapeutic applications against neoplastic, bacteria, viral, fungal and parasitic diseases. Additionally, they may be administered as a non-toxic adjuvant, in combination with chemotherapy. The soluble phosphorylated glucans are also useful for stimulating macrophage cells, either in vivo or in vitro, to produce a cytotoxic/cyctostatic factor effective against cancer cells.Type: GrantFiled: April 18, 1988Date of Patent: October 31, 1989Assignee: Bioglucans, L. P.Inventor: Nicholas R. DiLuzio
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Patent number: 4874851Abstract: The present invention provides novel 3',4'-dinitrogen substituted epipodophyllotoxin glucoside derivatives useful as antitumor agents.Type: GrantFiled: July 1, 1987Date of Patent: October 17, 1989Assignee: Bristol-Meyers CompanyInventors: Dolatrai M. Vyas, Mark G. Saulnier, John F. Kadow
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Patent number: 4873258Abstract: The present invention relates to antitumor compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monomethyl or monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 29 carbon atoms in total); ethers, esters thereof; acid addition salts thereof; wherein Ar is a fused tetracyclic aromatic ring system comprised of 5-membered and 6-membered rings and contains at least one heteroatom and 3 aromatic rings and a total of no more than 18 ring atoms, or a substituted derivative thereof; the heteroatom is preferably oxygen, sulfur or nitrogen; when it is nitrogen this is substituted by hydrogen, methyl or ethyl;R.sup.1 contains not more than eight carbon atoms and is a group ##STR1## wherein m is 0 or 1;R.sup.5 is hydrogen;R.sup.6 and R.sup.7 are the same or different and each is hydrogen or C.sub.1-5 alkyl optionally substituted by hydroxy;R.sup.8 and R.sup.9 are the same or different and each is hydrogen or C.sub.Type: GrantFiled: August 18, 1988Date of Patent: October 10, 1989Assignee: Burroughs Wellcome Co.Inventor: Kenneth W. Bair
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Patent number: 4868291Abstract: Novel 4'-deshydroxyepipodophyllotoxin glucosides are provided as antitumor agents useful in inhibiting the growth of mammalian tumors. The invention also provides novel intermediates and processes for the preparation of the 4'-deshydroxyepipodophyllotoxin glucoside end-products. A preferred embodiment is 4'-deshydroxyetoposide.Type: GrantFiled: August 20, 1987Date of Patent: September 19, 1989Assignee: Bristol-Myers CompanyInventors: Mark G. Saulnier, Dolatrai M. Vyas
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Patent number: 4866069Abstract: Disclosed are a compound of the general formula ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and each represents a hydrogen atom, an alkyl group or an acyl group, process for the production thereof and use thereof. The compounds have an antitumor activity, and those wherein both of R.sub.1 and R.sub.2 represent a hydrogen atom or an acyl group are novel compounds.Type: GrantFiled: October 3, 1988Date of Patent: September 12, 1989Assignee: Taiho Pharmaceutical Company, LimitedInventors: Qi Chang-qing, Tian Jie, Teruyoshi Marunaka, Yuji Yamada, Ichiro Yamawaki, Toshio Ohtani, Yoshinori Minami, Hitoshi Saito
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Patent number: 4863739Abstract: Disclosed are liposomal antitumor compositions having improved pharmacological characteristics. Liposomes described herein are formed through the incorporation of a particular class of anthracyclines, the 4-demethoxy-3'-desamino-2'-iodo analogs, shown to have extremely high incorporatio efficiencies of greater than 95%. These liposomes demonstrate an improved antitumor efficacy, with much reduced toxicity, against accepted tumor models, and further exhibit excellent stability upon storage, for example, in the form of a dried powder.Type: GrantFiled: May 19, 1987Date of Patent: September 5, 1989Assignee: Board of Regents, The University of Texas SystemInventors: Roman Perez-Soler, Waldemar Priebe, Gabriel Lopez-Berestein
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Patent number: 4855453Abstract: The present invention relates to anti tumor compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monomethyl or monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 29 carbon atoms in total); ethers, esters thereof; acid addition salts thereof; wherein Ar is a fused tetracyclic aromatic ring system comprised of 5-membered and 6-membered rings and contains at least one heteroatom and 3 aromatic rings and a total of no more than 18 ring atoms, or a substituted derivative thereof; the heteroatom is preferably oxygen, sulfur or nitrogen; when it is nitrogen this is substituted by hydrogen, methyl or ethyl;R.sup.1 contains not more than eight carbon atoms and is a group ##STR1## wherein m is 0 or 1;R.sup.5 is hydrogen;R.sup.6 and R.sup.7 are the same or different and each is hydrogen or C.sub.1-5 alkyl optionally substituted by hydroxy;R.sup.8 and R.sup.9 are the same or different and each is hydrogen or C.sub.Type: GrantFiled: May 16, 1988Date of Patent: August 8, 1989Assignee: Burroughs Wellcome Co.Inventor: Kenneth W. Bair
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Patent number: 4851437Abstract: Various tung oil or tung oil fatty acid compositions and use thereof for treating at least some symptoms of body defense deficiencies in patients having said symptoms.Type: GrantFiled: August 12, 1986Date of Patent: July 25, 1989Assignee: Elena AvramInventor: Emanuel Revici
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Patent number: 4829090Abstract: The present invention relates to compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monomethyl or a monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 30 carbon atoms in total); ethers, esters thereof; acid addition salts thereof; wherein Ar is a chrysene or substituted chrysene ring system; R.sup.1 contains not more than eight carbon atoms and is a group ##STR1## wherein m is 0 or 1;R.sup.5 is hydrogen;R.sup.6 and R.sup.7 are the same or different and each is hydrogen or C.sub.1-3 alkyl optionally substituted by hydroxy;R.sup.8 and R.sup.9 are the same or different and each is hydrogen or C.sub.1-3 alkyl; ##STR2## is a five- or six-membered saturated carbocyclic ring; R.sup.10 is hydrogen, methyl or hydroxymethyl;R.sup.11, R.sup.12 and R.sup.13 are the same or different and each is hydrogen or methyl;R.sup.14 is hydrogen, methyl, hydroxy, or hydroxymethyl.Type: GrantFiled: August 28, 1987Date of Patent: May 9, 1989Assignee: Burroughs Wellcome Co.Inventor: Kenneth W. Bair
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Patent number: 4820696Abstract: The use of mismatched dsRNA, e.g. Ampligen for the manufacture of compositions for use in the Selective activation of a latent natural defense system within human cells, both cells already infected with AIDS virus as well as cells at risk to infection. Specific treatments for various clinical phases of the biological continuum of AIDS virus-related events ranging from subtle, early immunological lesions to advanced disease are described. Prophylaxis or prevention of AIDS virus related events, such as by introduction of mismatched double-stranded RNA into various blood products of biological fluids to be used in man (e.g., blood transfusion) or around man (e.g., dialysis programs) are also described.Type: GrantFiled: September 30, 1988Date of Patent: April 11, 1989Assignee: HEM Research, Inc.Inventor: William A. Carter
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Patent number: 4814502Abstract: The present invention relates to compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monomethyl or monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 30 carbon atoms in total); ethers, esters, thereof; acid addition salts thereof; wherein Ar is a C.sub.15-18 fused tetracarbocyclic ring system containing 3 or 4 aromatic rings or a C.sub.17-22 fused pentacarbocyclic ring system containing 4, or 5 aromatic rings, or a substituted derivative thereof; the ring system Ar should be planar or deviate only slightly from planarity. Thus, the ring system contains a maximum of two non-aromatic carbon atoms which may be in the same ring, in which case they are adjacent, or in different rings;Ar is not perylene, fluoranthene, chrysene, pyrene, or triphenylene;R.sup.1 contains not more than eight carbon atoms and is a group ##STR1## wherein m is 0 or 1; R.sup.5 is hydrogen;R.sup.6 and R.sup.7 are the same or different and each is hydrogen or C.sub.Type: GrantFiled: January 19, 1988Date of Patent: March 21, 1989Assignee: Burroughs Wellcome Co.Inventor: Kenneth W. Bair
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Patent number: 4812449Abstract: Differences in microenvironments associated with various cells and other conditions in this environment are used to advantage in effecting the in situ construction of biologically active agents at target locations in preference to surroundings which are desired to be unaffected.Type: GrantFiled: October 14, 1987Date of Patent: March 14, 1989Assignee: Scripps Clinic and Research FoundationInventor: Darryl C. Rideout
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Patent number: 4810823Abstract: The present invention relates to compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monomethyl or monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 30 carbon atoms in total); ethers, esters, thereof; acid addition salts thereof; wherein Ar is a C.sub.15-18 fused tetracarbocyclic ring system containing 3 or 4 aromatic rings or a C.sub.17-22 fused pentacarbocyclic ring system containing 4, or 5 aromatic rings, or a substituted derivative thereof; the ring system Ar should be planar or deviate only slightly from planarity. Thus, the ring system contains a maximum of two non-aromatic carbon atoms which may be in the same ring, in which case they are adjacent, or in different rings;Ar is not perylene, fluoranthene, chrysene, pyrene, or triphenylene;R.sup.1 contains not more than eight carbon atoms and is a group ##STR1## wherein m is 0 or 1;R.sup.5 is hydrogen;R.sup.6 and R.sup.7 are the same or different and each is hydrogen or C.sub.Type: GrantFiled: December 21, 1987Date of Patent: March 7, 1989Assignee: Burroughs Wellcome Co.Inventor: Kenneth W. Bair
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Patent number: 4808632Abstract: The present invention relates to compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monomethyl or a monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 30 carbon atoms in total); ethers, esters thereof; acid addition salts thereof; wherein Ar is a fluoranthene or substituted fluoranthene ring system; R.sup.1 contains not more than eight carbon atoms and is a group ##STR1## wherein m is 0 or 1; R.sup.5 is hydrogen;R.sup.6 and R.sup.7 are the same or different and each is hydrogen or C.sub.1-3 alkyl optionally substituted by hydroxy;R.sup.8 and R.sup.9 are the same or different and each is hydrogen or C.sub.1-3 alkyl; ##STR2## is a five- or six-membered saturated carbocyclic ring; R.sup.10 is hydrogen, methyl or hydroxymethyl;R.sup.11, R.sup.12 and R.sup.13 are the same or different and each is hydrogen or methyl;R.sup.14 is hydrogen, methyl, hydroxy, or hydroxymethyl.Type: GrantFiled: July 30, 1987Date of Patent: February 28, 1989Assignee: Burroughs Wellcome Co.Inventor: Kenneth W. Bair
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Patent number: 4803226Abstract: The present invention relates to compounds of formula (I) ##STR1## wherein Ar is an anthracene or substituted anthracene ring system;R.sup.1 is a C.sub.1-3 alkylene moiety;R.sup.2 is hydrogen or a C.sub.1-6 alkyl group;R.sup.3 is a hydroxy C.sub.1-6 alkyl group;R.sup.4 and R.sup.5 are the same or different and are hydrogen, C.sub.1-6 alkyl or hydroxy C.sub.1-6 alkyl, esters thereof derived from condensation of carboxy acids and hydroxyl groups of R.sup.3, R.sup.4, and R.sup.5 ;Acid addition salts thereof, which have been found useful for the treatment of tumors in mammals.Type: GrantFiled: January 6, 1988Date of Patent: February 7, 1989Assignee: Burroughs Wellcome Co.Inventor: Kenneth W. Bair
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Patent number: 4803222Abstract: The present invention relates to compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monomethyl or a monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 30 carbon atoms in total); ethers, esters thereof; acid addition salts thereof; wherein Ar is a fluoranthene or substituted fluoranthene ring system; R.sup.1 contains not more than eight carbon carbon atoms and is a group ##STR1## wherein m is 0 or 1;R.sup.5 is hydrogen;R.sup.6 and R.sup.7 are the same or different and each is hydrogen or C.sub.1-3 alkyl optionally substituted by hydroxy;R.sup.8 and R.sup.9 are the same or different and each is hydrogen or C.sub.1-3 alkyl;--C--C-- is a five- or six-membered saturated carbocyclic ring;R.sup.10 is hydrogen, methyl or hydroxymethyl;R.sup.11, R.sup.12 and R.sup.13 are the same or different and each is hydrogen or methyl;R.sup.14 is hydrogen, methyl, hydroxy, or hydroxymethyl.Type: GrantFiled: August 28, 1987Date of Patent: February 7, 1989Assignee: Burroughs Wellcome Co.Inventor: Kenneth W. Bair
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Patent number: 4803221Abstract: The present invention relates to compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monomethyl or a monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 30 carbon atoms in total); ethers, esters thereof; acid addition salts thereof; wherein Ar is an anthracene or substituted anthracene ring system; R.sup.1 contains not more than eight carbon atoms and is a group ##STR1## wherein m is 0 or 1;R.sup.5 is hydrogen;R.sup.6 and R.sup.7 are the same or different and each is hydrogen or C.sub.1-3 alkyl optionally substituted by hydroxy;R.sup.8 and R.sup.9 are the same or different and each is hydrogen or C.sub.1-3 alkyl; ##STR2## is a five- or six-membered saturated carbocyclic ring; R.sup.10 is hydrogen, methyl or hydroxymethyl;R.sup.11, R.sup.12 and R.sup.13 are the same or different and each is hydrogen or methyl;R.sup.14 is hydrogen, methyl, hydroxy, or hydroxymethyl.Type: GrantFiled: August 28, 1987Date of Patent: February 7, 1989Assignee: Burroughs Wellcome Co.Inventor: Kenneth W. Bair
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Patent number: 4797495Abstract: The present invention relates to compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monomethyl or monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 29 carbon atoms in total); ethers, esters thereof; acid addition salts thereof; wherein Ar is a fused tetracyclic aromatic ring system comprised of 5-membered and 6-membered rings and contains at least one heteroatom and 3 aromatic rings and a total of no more than 18 ring atoms, or a substituted derivative thereof; the heteroatom is preferably oxygen, sulfur or nitrogen; when it is nitrogen this is substituted by hydrogen, methyl or ethyl;R.sup.1 contains not more than eight carbon atoms and is a group ##STR1## wherein m is 0 or 1; R.sup.5 is hydrogen;R.sup.6 and R.sup.7 are the same or different and each is hydrogen or C.sub.1-5 alkyl optionally substituted by hydroxy;R.sup.8 and R.sup.9 are the same or different and each is hydrogen or C.sub.Type: GrantFiled: December 4, 1987Date of Patent: January 10, 1989Assignee: Burroughs Wellcome Co.Inventor: Kenneth W. Bair
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Patent number: 4795812Abstract: This invention describes the synthesis and anti-neoplastic use of 4-aziridyl-5-substituted/unsubstituted 6-aryl-pyrimidine compounds of Formula IA ##STR1## as well as N'-[2-(1-aziridyl)ethyl]-6-aryl-2,4-pyrimidinediamines of Formula IB ##STR2## and 4-chloro or bromo-5-substituted/unstubstituted-6-aryl-pyrimidines.Type: GrantFiled: September 22, 1986Date of Patent: January 3, 1989Assignee: The Upjohn CompanyInventors: Wendell Wierenga, Harvey I. Skulnick
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Patent number: 4794114Abstract: A method of inhibiting the 5-lipoxygenase pathway in an animal in need thereof which comprises administering an effective, 5-lipoxygenase pathway inhibiting amount of a diaryl-substituted imidazole fused to a thiazole pyrrolidine, thiazide or piperidine ring to such animal.Type: GrantFiled: June 17, 1987Date of Patent: December 27, 1988Assignee: SmithKline Beckman CorporationInventors: Paul E. Bender, Don E. Griswold, Nabil Hanna, John C. Lee
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Patent number: 4791233Abstract: The present invention relates to compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monomethyl or monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 30 carbon atoms in total); ethers, esters, thereof; acid addition salts thereof; wherein Ar is a C.sub.15-18 fused tetracarbocyclic ring system containing 3 or 4 aromatic rings or a C.sub.17-22 fused pentacarbocyclic ring system containing 4, or 5 aromatic rings, or a substituted derivative thereof; the ring system Ar should be planar or deviate only slightly from planarity. Thus, the ring system contains a maximum of two non-aromatic carbon atoms which may be in the same ring, in which case they are adjacent, or in different rings;Ar is not perylene, fluoranthene, chrysene, pyrene, or triphenylene;R.sup.1 contains not more than eight carbon atoms and is a group ##STR1## wherein m is 0 or 1;R.sup.5 is hydrogen;R.sup.6 and R.sup.7 are the same or different and each is hydrogen or C.sub.Type: GrantFiled: January 19, 1988Date of Patent: December 13, 1988Assignee: Burroughs Wellcome Co.Inventor: Kenneth W. Bair
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Patent number: 4791232Abstract: The present invention relates to compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monomethyl or monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 30 carbon atoms in total); ethers, esters, thereof; acid addition salts thereof; wherein Ar is a C.sub.15-18 fused tetracarbocyclic ring system containing 3 or 4 aromatic rings or a C.sub.17-22 fused pentacarbocyclic ring system containing 4, or 5 aromatic rings, or a substituted derivative thereof; the ring system Ar should be planar or deviate only slightly from planarity. Thus, the ring system contains a maximum of two non-aromatic carbon atoms which may be in the same ring, in which case they are adjacent, or in different rings;Ar is not perylene, fluoranthene, chrysene, pyrene, or triphenylene;R.sup.1 contains not more than eight carbon atoms and is a group ##STR1## wherein m is 0 or 1; R.sup.5 is hydrogen;R.sup.6 and R.sup.7 are the same or different and each is hydrogen or C.sub.Type: GrantFiled: January 19, 1988Date of Patent: December 13, 1988Assignee: Burroughs Wellcome Co.Inventor: Kenneth W. Bair
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Patent number: 4791231Abstract: The present invention relates to compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monomethyl or monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 30 carbon atoms in total); ethers, esters, thereof; acid addition salts thereof; wherein Ar is a C.sub.15-18 fused tetracarbocyclic ring system containing 3 or 4 aromatic rings or a C.sub.17-22 fused pentacarbocyclic ring system containing 4, or 5 aromatic rings, or a substituted derivative thereof; the ring system Ar should be planar or deviate only slightly from planarity. Thus, the ring system contains a maximum of two non-aromatic carbon atoms which may be in the same ring, in which case they are adjacent, or in different rings;Ar is not perylene, fluoranthene, chrysene, pyrene, or triphenylene;R.sup.1 contains not more than eight carbon atoms and is a group ##STR1## wherein m is 0 or 1; R.sup.5 is hydrogen;R.sup.6 and R.sup.7 are the same or different and each is hydrogen or C.sub.Type: GrantFiled: January 19, 1988Date of Patent: December 13, 1988Assignee: Burroughs Wellcome Co.Inventor: Kenneth W. Bair
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Patent number: 4783454Abstract: A new pharmaceutical composition for treating nonlymphatic leukemia, such as granulocytic and monocytic leukemia comprising Harringtonine, Homoharringtonine, Anethole, Oleanolic acid and Ginsenoside and method of making the same.Type: GrantFiled: May 14, 1987Date of Patent: November 8, 1988Inventor: Yaguang Liu
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Patent number: 4769453Abstract: The present invention relates to a process for the preparation of bis-indolic compounds, and the bis-indolic compounds produced by the process.Type: GrantFiled: June 18, 1981Date of Patent: September 6, 1988Assignee: Agence Nationale de Valorisation de la RechercheInventors: Pierre Potier, Nicole Langlois, Yves Langlois, Francoise Gueritte
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Patent number: 4769250Abstract: Formulations consisting of phospholipid bilayer membrane particles made from mixtures of anionic and neutral phospholipids encapsulating anthracycline anti-neoplastic agents, suspended in a low ionic strength aqueous phase, are described. In a preferred embodiment, the particles are in the form of vesicles which comprise daunorubicin, distearoyl phosphatidylglycerol and distearoyl phosphatidylcholine, the mol ratio of daunorubicin to distearoyl phosphatidylglycerol is at least about 1:1.25, and the suspending medium is an aqueous lactose solution containing a small amount of base.Type: GrantFiled: October 26, 1987Date of Patent: September 6, 1988Assignee: Vestar, Inc.Inventor: Eric A. Forssen
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Patent number: 4767872Abstract: A compound of the formula ##STR1## wherein R.sub.1 and R.sub.2 each independently represent a hydrocarbon gp which can be substituted and/or carry a heteroatom, or R.sub.1 and R.sub.2 together represent a hydrocarbon, optionally substituted, forming with the carbon atom to which they are attached, a ring capable of carrying a heteroatom, R.sub.3 represents hydrogen, lower alkyl or aryl, and R.sub.4 and R.sub.5 each independently represent hydrogen or a hydrocarbon group, as well as the acid addition salts thereof. A method of preparing the compounds and the use thereof as an anti-tumor medicine are disclosed.Type: GrantFiled: January 31, 1986Date of Patent: August 30, 1988Assignees: Centre National de la Recherche Scientifique (CNRS), Institut National de la Sante et de la Recherche Medicale (INSERM)Inventors: Alain Doutheau, Jacques Gore, Gerard A. Quash, Bernard Didier
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Patent number: 4720543Abstract: This invention discloses 1a- and 7-substituted derivatives of mitosanes containing thiocarbamoyl and glycosyl residues. The compounds possess antibacterial and antitumor activity, with a concomitant reduction in bone marrow toxicity as compared to the parent compounds.Type: GrantFiled: June 6, 1985Date of Patent: January 19, 1988Assignee: Georgetown UniversityInventors: Eugene McPherson, Philip S. Schein
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Patent number: 4720587Abstract: The present invention relates to compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monomethyl or a monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 30 carbon atoms in total); ethers, esters thereof; acid addition salts thereof; wherein Ar is a fluoranthene or substituted fluoranthene ring system; R.sup.1 contains not more than eight carbon carbon atoms and is a group ##STR1## wherein m is 0 or 1;R.sup.5 is hydrogen;R.sup.6 and R.sup.7 are the same or different and each is hydrogen or C.sub.1-3 alkyl optionally substituted by hydroxy;R.sup.8 and R.sup.9 are the same or different and each is hydrogen or C.sub.1-3 alkyl; ##STR2## is a five- or six-membered saturated carbocyclic ring; R.sup.10 is hydrogen, methyl or hydroxymethyl;R.sup.11, R.sup.12 and R.sup.13 are the same or different and each is hydrogen or methyl;R.sup.14 is hydrogen, methyl, hydroxy, or hydroxymethyl.Type: GrantFiled: October 17, 1984Date of Patent: January 19, 1988Assignee: Burroughs Wellcome Co.Inventor: Kenneth W. Bair
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Patent number: 4719236Abstract: The present invention relates to compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monomethyl or a monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 30 carbon atoms in total); ethers, esters thereof; acid additon salts thereof; wherein Ar is a perylene or substituted perylene ring system; R.sup.1 contains not more than eight carbon carbon atoms and is a group ##STR1## wherein m is 0 or 1;R.sup.5 is hydrogen;R.sup.6 and R.sup.7 are the same or different and each is hydrogen or C.sub.1-3 alkyl optionally substituted by hydroxy;R.sup.8 and R.sup.9 are the same or different and each is hydrogen or C.sub.1-3 alkyl; ##STR2## is a five- or six-membered saturated carbocyclic ring; R.sup.10 is hydrogen, methyl or hydroxymethyl;R.sup.11, R.sup.12 and R.sup.13 are the same or different and each is hydrogen or methyl; R.sup.14 is hydrogen, methyl, hydroxy, or hydroxymethyl.Type: GrantFiled: October 17, 1984Date of Patent: January 12, 1988Assignee: Burroughs Wellcome Co.Inventor: Kenneth W. Bair
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Patent number: 4717729Abstract: The present invention relates to compounds of formula (I) ##STR1## wherein Ar is a triphenylene or substituted triphenylene ring system;R.sup.1 is a C.sub.1-3 alkylene moiety;R.sup.2 is hydrogen or a C.sub.1-6 alkyl group;R.sup.3 is a hydroxy C.sub.1-6 alkyl group;R.sup.4 and R.sup.5 are the same or different and are hydrogen, C.sub.1-6 alkyl or hydroxy C.sub.1-6 alkyl, esters thereof derived from condensation of carboxylic acids and hydroxyl groups of R.sup.3, R.sup.4, and R.sup.5 ;Acid addition salts thereof, which have been found useful for the treatment of tumors in mammals.Type: GrantFiled: September 5, 1985Date of Patent: January 5, 1988Assignee: Burroughs Wellcome Co.Inventor: Kenneth W. Bair
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Patent number: 4698423Abstract: An ellipticine derivative having the structure: ##STR1## as well as process for the preparation of such ellipticine derivatives. The ellipticine derivatives have antineoplastic or antitumor activity.Type: GrantFiled: July 25, 1985Date of Patent: October 6, 1987Assignee: Suntory LimitedInventors: Tadashi Honda, Toshihiro Nakanishi
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Patent number: 4684521Abstract: A chemical agent is disclosed which is useful for reducing the population of a selected blood constituent having receptor sites. The chemical agent includes a carrier having a strong affinity for the receptor sites on the blood constituent and a photoactive agent physically incorporated within or chemically bound to the carrier moiety which interferes with the metabolism of the selected blood constituent when activated by UV radiation. The photoactive agent may be a photocytotoxin selected from the group consisting of psoralen, pyrene, cholesteryloleate, acridine, porphyrin, fluorescein, rhodamine, 16-diazocortisone, ethidium, transistion metal complexes of bleomycin, transition metal complexes of deglycobleomycin and organoplatinum complexes.Type: GrantFiled: June 21, 1985Date of Patent: August 4, 1987Assignees: Frederic A. Bourke, Jr., Eleanor F. Bourke, Richard L. EdelsonInventor: Richard L. Edelson
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Patent number: 4665201Abstract: Novel antineoplastic ailanthone derivatives (IIb) represented by the following formula wherein R.sub.2 is C.sub.5 -C.sub.18 .alpha.,.beta.-unsaturated acyl group and its related compounds are disclosed. ##STR1## Particularly, some of the above compounds are far more effective than mitomycin C against mouse lymphocytic leucemia p388.These compounds can be synthesized from known ailanthone via important intermediates, triacyloxy ailanthone, represented by the formula: ##STR2## wherein R.sub.1 is acyl group.Type: GrantFiled: January 15, 1985Date of Patent: May 12, 1987Assignee: Suntory, LimitedInventors: Tadashi Honda, Kayoko Imao, Nobuo Nakatsuka, Toshihiro Nakanishi
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Patent number: 4636508Abstract: Novel 5-pyrimidinecarboxamides useful for regressing or inhibiting the growth of leukemia and tumors. The compounds have the formula: ##STR1## wherein R.sub.1 is hydrogen or an alkoxy group having from one to four carbon atoms;R.sub.2 is hydrogen; alkyl, aryl, aralkyl, allyl, aralkenyl or aralkynyl, the alkyl, alkenyl or alkynyl moieties of which have from one to six carbon atoms, or a carbohydrate residue;R.sub.3 is hydrogen, C.sub.1 -C.sub.4 alkyl or aryl;R.sub.Type: GrantFiled: April 22, 1985Date of Patent: January 13, 1987Assignees: Uniroyal Chemical Company, Inc., Uniroyal Ltd.Inventors: Arthur D. Brewer, John A. Minatelli
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Patent number: 4621086Abstract: Pyrazolo[3,4,5-kl]acridines are described as antibacterial agents and antitumor agents as well as pharmaceutical compositions and methods for their preparation.Type: GrantFiled: January 22, 1986Date of Patent: November 4, 1986Assignee: Warner-Lambert CompanyInventor: David B. Capps
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Patent number: 4590277Abstract: 4-Carboxamidoacridine compounds represented by the general formula (I), ##STR1## where R.sub.1 represents H, CH.sub.3 or NHR.sub.3, where R.sub.3 is H, COCH.sub.3, SO.sub.2 CH.sub.3, COPh, SO.sub.2 Ph or lower alkyl optionally substituted with hydroxyl and/or amino functions;R.sub.2 represents H or up to two of the groups CH.sub.3, OCH.sub.3, halogen, CF.sub.3, NO.sub.2, NH.sub.2, NHCOCH.sub.3, and NHCOOCH.sub.3 placed at positions 1-3 or 5-8;Y represents C(NH)NH.sub.2, NHC(NH)NH.sub.2, or NR.sub.4 R.sub.5, where each of R.sub.4 and R.sub.5 is H or lower alkyl optionally substituted with hydroxyl and/or amino functions; andx is from 2 to 6,and the acid addition salts thereof, possess antibacterial and antitumor properties.Type: GrantFiled: June 21, 1983Date of Patent: May 20, 1986Assignee: Development Finance Corporation of New ZealandInventors: Graham J. Atwell, Bruce C. Baguley, William A. Denny, Gordon W. Rewcastle
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Patent number: 4576948Abstract: New uracil compounds having the formula: ##STR1## wherein X is C.sub.1 -C.sub.10 alkoxy or amino are provided. These compounds are useful in treating patients having leukemia, the cells of which express terminal deoxynucleootidyl transferase.Type: GrantFiled: January 20, 1983Date of Patent: March 18, 1986Assignee: Trustees Boston UniversityInventors: Ronald McCaffrey, George Wright, Earl F. Baril
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Patent number: 4575509Abstract: This invention concerns novel water-soluble salts and compositions of the antitumor agent 4'-(9-acridinylamino) methanesulfon-m-anisidide (m-AMSA). More particularly, there are provided (1) the mono- and dipyroglutamate salts of m-AMSA and (2) compositions of m-AMSA with pyroglutamic acid. The novel salts and compositions provided enable m-AMSA to be administered as an aqueous solution without the necessity of using dimethylacetamide as a pharmaceutical vehicle.Type: GrantFiled: July 18, 1984Date of Patent: March 11, 1986Assignee: Bristol-Myers CompanyInventors: Jivn-Ren Chen, Edward C. Shinal
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Patent number: 4562204Abstract: Trans-.DELTA..sup.2 -prostaglandin D derivatives of the formula: ##STR1## wherein [A] is a group of the formula: ##STR2## X is ethylene or cis-vinylene, C.sub.13 -C.sub.14 -C.sub.15 is: (i) a group of the formula: ##STR3## when [A] is a group of the formula (II) or (III), or (ii) a group of the formula: ##STR4## when [A] is a group of the formula (IV), R is hydrogen or alkyl, R.sup.1 is a single bond or alkylene, R.sup.2 is alkyl, cycloalkyl, phenyl or phenoxy, the double bonds between C.sub.2 -C.sub.3 and between C.sub.13 -C.sub.14 are both E, the double bond between C.sub.9 -C.sub.10 is Z and the double bonds between C.sub.12 -C.sub.13 and between C.sub.14 -C.sub.15 are E, Z or a mixture thereof, provided that when R.sup.1 is a single bond, R.sup.2 does not represent a substituted or unsubstituted phenoxy group, and cyclodextrin clathrates and non-toxic salts thereof, possess anti-tumor activity.Type: GrantFiled: June 28, 1983Date of Patent: December 31, 1985Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Hirohisa Wakatsuka, Takashi Yamato, Shinsuke Hashimoto
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Patent number: 4542219Abstract: Ethylene glycol derivatives, inclusive of salts thereof, which have the formula: ##STR1## wherein R.sup.1 is C.sub.8-26 aliphatic hydrocarbon residue; R.sup.2, R.sup.3 and R.sup.4 are each hydrogen or lower alkyl which may be substituted, or --N.sup.+ R.sup.2 R.sup.3 R.sup.4 represents cyclic ammonio, exhibit inhibitory activity to multiplication of tumor cells and antimicrobial activity.Type: GrantFiled: March 24, 1982Date of Patent: September 17, 1985Assignee: Takeda Chemical Industries, Ltd.Inventors: Motoo Hozumi, Hiroaki Nomura, Yoshio Yoshioka