Tetracyclo Ring System Having The Lactone Ring As One Of The Cyclos Patents (Class 549/298)
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Patent number: 7087641Abstract: The present invention provides a new class of compounds 4?-1?-[{2?-benzoyl substituted}anilino] podophyllotoxin exhibiting anti cancer activity and a process for preparing the same.Type: GrantFiled: March 28, 2002Date of Patent: August 8, 2006Assignee: Council of Scientific & Industrial ResearchInventors: Ahmed Kamal, Peram Surakattula Murali Mohan Reddy
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Patent number: 7019151Abstract: Compounds having the structure I: are useful for inducing cell death (apoptosis) and in immunosuppression. In structure I, R1 is H or R, R being selected from lower alkyl, alkenyl, alkynyl, and allenyl, or, R1 together with R2=O (oxo); R2=OH, or, R1 and R2 together=O (oxo); CR3R5 and CR4R6 are selected from CH2, CHOH and CROH; at least one of R1, R5 and R6 is R; and at least one of CR3R5 and CR4R6 is CH2.Type: GrantFiled: December 16, 2003Date of Patent: March 28, 2006Assignee: Pharmagenesis, Inc.Inventors: Dongcheng Dai, John H. Musser
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Patent number: 6903133Abstract: This invention features compounds having formula (I): wherein, R1, R2, R3, R4, R5, R6, R7, T, X, and Y are as defined herein. This invention also features a method for treating cancer. The method includes administrating to a subject in need thereof a compound of formula (I).Type: GrantFiled: October 14, 2003Date of Patent: June 7, 2005Assignee: Plantaceutica, Inc.Inventors: Qian Shi, Hui-Kang Wang, Masayoshi Oyama, John Robert Vance, Ming S. Chen
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Patent number: 6894075Abstract: The present invention provides a novel 4?-demethyl-4?-O-substituted-1-deoxypodophyllotoxin derivative, a geometric isomer thereof, a process for the preparation thereof, and an anticancer composition comprising the same.Type: GrantFiled: November 19, 2001Date of Patent: May 17, 2005Inventors: Song-Bae Kim, Byung-Zun Ahn, Yong Kim, Young-Jae You
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Patent number: 6887869Abstract: The invention concerns novel mikanolide derivatives, their preparation method and their therapeutic uses, in particular as anti-cancer and anti-viral agents.Type: GrantFiled: January 11, 2002Date of Patent: May 3, 2005Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)Inventors: Olivier Lavergne, Christophe Lanco, Grégoire Prevost, Beng Poon Teng
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Patent number: 6878746Abstract: A compound selected from these of formula (I): wherein: R1 represents hydrogen, alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, alkoxycarbonyl, aryloxycarbonyl, arylalkoxycarbonyl, heterocycloalkoxycarbonyl, alkylsulfonyl, arylsulfonyl, arylalkylsulfonyl or phosphono, R2 represents oxygen or sulphur, R3 represents hydrogen or alkyl, cycloalkyl or arylalkyl, X represents linear or branched (C1-C6)alkylene, R4 represents a group selected from amino optionally substituted by one or two groups, —N(R3)—X1—OR5 wherein R3, X1 and R5 are as defined in the description, —N(R3)—X1—NR6R7 wherein R3, X1, R6 and R7 are as defined in the description, hydroxy, alkoxy, aryloxy, —O—X1—OR5 wherein R5 and X1 are as defined in the description, and —O—X1—NR6R7 wherein R6, R7 and X1 are as defined in the description, its isomers, and also addition salts thereof with a pharmaceutically acceptable acid or base, and medical products containing the same which are useful in the treatment of cancer.Type: GrantFiled: June 19, 2001Date of Patent: April 12, 2005Assignee: Les Laboratoires ServierInventors: Claude Monneret, Emmanuel Bertounesque, Philippe Meresse, Ghanem Atassi, Alain Pierre, John Hickman, Bruno Pfeiffer, Pierre Renard
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Patent number: 6872838Abstract: The present invention is directed to novel water-soluble prodrugs of aliphatic or aromatic hindered hydroxyl group containing pharmaceuticals.Type: GrantFiled: July 29, 2002Date of Patent: March 29, 2005Assignee: University of KansasInventors: Valentino J. Stella, Jan J. Zygmunt, Ingrid Gunda Georg, Muhammad S. Safadi
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Patent number: 6861537Abstract: The synthesis of taxol and other tricyclic and tetracyclic taxanes.Type: GrantFiled: July 12, 2002Date of Patent: March 1, 2005Assignee: Florida State UniversityInventors: Robert A. Holton, Carmen Somoza, Hyeong Baik Kim, Mitsuru Shindo, Ronald J. Biediger, P. Douglas Boatman, Chase Smith, Feng Liang, Krishna Murthi
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Patent number: 6844451Abstract: A method of isolating terpene trilactones from Ginkgo biloba plant material or extract comprising the steps of suspending the plant material or extract in either water or an aqueous solution of an oxidation reagent; extracting the terpene trilactones using an acceptable extraction agent; separating the organic layer from the aqueous layer; washing the organic layer with an acceptable aqueous salt or hydroxide solution, which may be an alkaline solution; and drying the organic layer to form a dried extract containing terpene trilactones. Further purification by treatment with or filtration over activated charcoal, by treatment with or filtration over alumina and by recrystallization with an acceptable solvent or solvent mixture leads to extracts with a content of terpene trilactones higher than 50%. Unwanted levels of ginkgolic acids are reduced to acceptable levels by reversed phase chromatography.Type: GrantFiled: July 7, 2003Date of Patent: January 18, 2005Assignee: The Trustees of Columbia University in the City of New YorkInventors: Dirk Lichtblau, Nina Berova, John Berger, Koji Nakanishi
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Publication number: 20040186169Abstract: The invention refers to the use of specific cyclolignans, wherein the carbon atoms in positions 9 and 9′ have cis configuration, for inhibition of the insulin-like growth factor-1 receptor. Said compounds can be used for treatment of IGF-IR dependent diseases, such as cancer, psoriasis, artherosclerosis and acromegaly. A preferred compound is picropodophyllin.Type: ApplicationFiled: December 19, 2003Publication date: September 23, 2004Inventors: Olle Larsson, Magnus Axelson
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Publication number: 20040122084Abstract: The invention concerns novel mikanolide derivatives, their preparation method and their therapeutic uses, in particular as anti-cancer and anti-viral agents. The compounds correspond to general formula (1) corresponding to general sub-formulae (I)1 and (I)2, wherein: R1 represents H, SR4 or NR4R5; R2 represents SR6 or NR6R7; R3 represents OH, O(CO)R14, OSiR15R16R17, O(CO)OR18 or O(CO)NHR18, each of the radicals R4, R6, R15, R16 and R17 representing independently (in particular) an alkyl radical, the radicals R5 and R7 representing (in particular) radicals selected independently among a hydrogen atom and an alkyl radical, and each of the radicals R14 and R18 representing independently (in particular) an alkyl or cycloalkyl radical, or one among aryl, heteroaryl, aralkyl or heteroalkyl radicals optionally substituted; provided that when the compounds correspond to the general sub-formula (I)2, then R1 does not represent a hydrogen atom.Type: ApplicationFiled: June 25, 2003Publication date: June 24, 2004Inventors: Olivier Lavergne, Christophe Lanco, Gregoire Prevost, Beng Poon Teng
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Publication number: 20040106676Abstract: Etoposide analogs with improved water-solubility such as 4′-O-Demethyl-4′-(N′,N′-dimethyl-glycyl)-4&bgr;-(4″-nitroanilino)-4-desoxy-podophyllotoxin (8) and 4′-O-Demethyl-4′-(N′,N′-dimethyl-glycyl)-4&bgr;-(4″-fluoroanilino)-4-desoxy-podophyllotoxin (9) are described, along with pharmaceutical formulations containing the same, methods of use thereof, and intermediates and methods of making the same.Type: ApplicationFiled: November 13, 2003Publication date: June 3, 2004Inventors: Kuo-Hsiung Lee, Zhiyan Xiao, Kenneth F. Bastow
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Publication number: 20040101574Abstract: Compounds of formula (I): 1Type: ApplicationFiled: December 20, 2002Publication date: May 27, 2004Inventors: Claude Monneret, Emmanuel Bertounesque, Philippe Meresse, Ghanem Atassi, Alain Pierre, John Hickman, Bruno Pfeiffer, Pierre Renard
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Patent number: 6713454Abstract: The present invention provides amphiphilic prodrugs comprising a therapeutic compound conjugated to an PEG-oligomer/polymer and methods for using said prodrugs to enable oral drug delivery and/or delivery of drugs across the blood brain barrier into the central nervous system.Type: GrantFiled: December 31, 1999Date of Patent: March 30, 2004Assignee: Nobex CorporationInventors: Nnochiri Ekwuribe, Christopher H. Price, Tatyana A. Dyakonov
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Publication number: 20040044058Abstract: The present invention provides a novel 4′-demethyl-4′-O-substituted-1-deoxypodophyllotoxin derivative, a geometric isomer thereof, a process for the preparation thereof, and an anticancer composition comprising the same.Type: ApplicationFiled: April 28, 2003Publication date: March 4, 2004Inventors: Song-Bae Kim, Byung-Zun Ahn, Yong Kim, Young-Jae You
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Patent number: 6693091Abstract: A compound having the structure: wherein R1 is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; wherein R2 is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; wherein R3 is H or OH; wherein R4 is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; and wherein at least one of R1, R2, R3, or R4 is a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety. Optically pure enantiomers and salts of the compound are also described. Also, the synthesis of the compound, and uses of the compound, such as in a method for detecting the localization of, or identifying, receptors, enzymes or other targets, whether in a cell or in a subject.Type: GrantFiled: March 29, 2002Date of Patent: February 17, 2004Assignee: The Trustees of Columbia University in the City of New YorkInventors: Kristian Stromgaard, Makiko Suehiro, Koji Nakanishi
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Publication number: 20040006126Abstract: Etoposide analogs such as 4′-O-demethyl-4&bgr;-[4″-(methyl-L-tyrosine-N-carbonyl)-anilino]-4-desoxy-podophyllotoxin (12) and 4′-O-demethyl-4&bgr;-[4″-(methyl-L-tryptophan-N-carbonyl)-anilino]-4-desoxypodophyllotoxin (13) are described, along with pharmaceutical formulations containing the same, methods of use thereof, and intermediates and methods of making the same.Type: ApplicationFiled: January 22, 2003Publication date: January 8, 2004Inventors: Kuo-Hsiung Lee, Zhiyan Xiao, Kenneth F. Bastow
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Publication number: 20040006121Abstract: This invention provides a total synthesis of Merrillactone and Merrilactone analogues having the structure 1Type: ApplicationFiled: December 13, 2002Publication date: January 8, 2004Inventors: Samuel J. Danishefsky, Vladimir B. Birman
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Patent number: 6590109Abstract: A method of isolating terpene trilactones from Ginkgo biloba plant material or extract comprising the steps of suspending the plant material or extract in either water or an aqueous solution of an oxidation reagent; extracting the terpene trilactones using an acceptable extraction agent; separating the organic layer from the aqueous layer; washing the organic layer with an acceptable aqueous salt or hydroxide solution, which may be an alkaline solution; and drying the organic layer to form a dried extract containing terpene trilactones. Further purification by treatment with or filtration over activated charcoal, by treatment with or filtration over alumina and by recrystallization with an acceptable solvent or solvent mixture leads to extracts with a content of terpene trilactones higher than 50%. Unwanted levels of ginkgolic acids are reduced to acceptable levels by reversed phase chromatography.Type: GrantFiled: July 11, 2002Date of Patent: July 8, 2003Assignee: The Trustees of Columbia University in the City of New YorkInventors: Dirk Lichtblau, Nina Berova, John Berger, Koji Nakanishi
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Patent number: 6566393Abstract: Etoposide analogs such as 4′-O-demethyl-4&bgr;-[4″-(methyl-L-tyrosine-N-carbonyl)-anilino]-4-desoxy-podophyllotoxin (12) and 4′-O-demethyl-4&bgr;-[4″-(methyl-L-tryptophan-N-carbonyl)-anilino]-4-desoxypodophyllotoxin (13) are described, along with pharmaceutical formulations containing the same, methods of use thereof, and intermediates and methods of making the same.Type: GrantFiled: June 21, 2002Date of Patent: May 20, 2003Assignee: The University of North Carolina at Chapel HillInventors: Kuo-Hsiung Lee, Zhiyan Xiao, Kenneth F. Bastow
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Patent number: 6476251Abstract: The present invention relates to a novel process for preparing compounds of the formula (I) by reacting compounds of the formula (II) with a base and compounds of the formula (III) in which X, Y, Z, n, G, A, B, R1, R8 and Hal are each as defined above.Type: GrantFiled: March 12, 2001Date of Patent: November 5, 2002Assignees: Bayer Aktiengesellschaft, Bayer CorporationInventor: Volker Falbe
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Patent number: 6441198Abstract: The present invention discloses novel podophyllotoxin dimers having structural formula I wherein R is H or CH3 and Z is aryl or subsituted aryl compound selected form the group counting of phenylene, naphthalene, p-terpbhnyl, dimethoxy benzidine and diphenyl ether and a process for the preparation of said novel podophyllotoxin dimers. The new podophyllotoxin dimers, pawculaty 4-arylamino derivatives of the podophyllotoxin dimers of the present invention as useful as potent inhibitors of DNA-topoisomerase II and are also useful as antitumour agents.Type: GrantFiled: December 22, 2000Date of Patent: August 27, 2002Assignee: Council of Scientific and Industrial ResearchInventors: Ahmed Kamal, Laxman Eltepu, Arifuddin Mohammed, Gollapalli Bhasker Ramesh Khanna
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Publication number: 20020082432Abstract: The present invention discloses novel podophyllotoxin dimers having structural formula I 1Type: ApplicationFiled: December 22, 2000Publication date: June 27, 2002Applicant: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCHInventors: Ahmed Kamal, Laxman Eltepu, Arifuddin Mohammed, Gollapalli Bhasker Ramesh Khanna
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Patent number: 6395711Abstract: The compound referred to herein as IB-962 12, having structure (I) can be obtained by cultivating the strain of Micromonospora sp. ES25-008, available under the accession number CECT-3333, and can be hydrolyzed to give IB-96212B having structure (II). The sugar substituent which is L-rhodinose, can its elf be derivatized or the sugar can be replaced, in either case, giving further derivatives of IB-96212 having a group other than L-rhodinose at the position of the sugar.Type: GrantFiled: April 17, 2000Date of Patent: May 28, 2002Assignee: Instituto Biomar S.A.Inventors: Rosa Isabel Fernandez-Chimeno, Francisco Romero, Jose Luis Fernandez-Puentes, Julia Perez-Baz, Librada Maria Canedo, Fernando Espliego
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Patent number: 6392059Abstract: Intermediates for the preparation of himbacine exhibiting muscarinic M2 receptor antagonism, which are hydronaphtho[2,3-c]furan derivatives represented by general formula (1) or intermediates for the preparation thereof: wherein R1 is lower alkyl or aralky; R2 is hydrogen, lower alkyl or aralkyl; R3 and R4 together represent oxygen or methylene, or alternatively R4 is hydroxyl, lower alkoxy, aralkyloxy or lower acyloxy, with R3 being hydrogen; R5 and R6 together represent oxygen, or alternatively R6 is hydroxyl, lower alkxy, aralkyloxy or lower acyloxy, with R5 being hydrogen; and either of the broken lines is a single bond and the other thereof is a double bond, or alternatively both are single bonds.Type: GrantFiled: June 7, 2001Date of Patent: May 21, 2002Assignees: Sagami Chemical Reasearch Center, Kyorin Pharmaceutical Co., Ltd.Inventors: Shiro Terashima, Masanori Takadoi, Akihiro Ishiwata, Tadashi Katoh
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Patent number: 6387948Abstract: 8-Acetylarteminolide of the formula (I) having inhibitory activities against farnesyl-protein transferase(FPTase), a progression of the cell cycle and angiogenesis may be useful for the prevention and treatment of various cancers and angiogenesis-related diseases:Type: GrantFiled: June 17, 2000Date of Patent: May 14, 2002Assignee: Korea Research Institute of Bioscience and BiotechnologyInventors: Byoung-Mog Kwon, Kwang-Hee Son, Ha-Won Jeong, Seung-Ho Lee, Mi-Young Han, Hyun-Mi Kang, Hyae-Kyeong Kim, Soo-Ik Chang
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Patent number: 6380257Abstract: The present invention relates to new aromatic di-keto derivatives and to their pharmaceutically acceptable salts, esters, ethers and other chemical equivalents. The derivatives are glucose-6-phosphate translocase inhibitors and can be used in the treatment of diabetes mellitus. The present invention further relates to a process for the production of the derivatives, to the use of the derivatives and their pharmaceutically acceptable salts, esters, ethers and other chemical equivalents as pharmaceuticals, in particular to their use in the treatment of diabetes mellitus, and to pharmaceutical compositions comprising the derivatives, pharmaceutically acceptable salts, esters, ethers or other chemical equivalents thereof.Type: GrantFiled: October 24, 2000Date of Patent: April 30, 2002Assignee: Aventis Pharma Deutschland GmbHInventors: László Vértesy, Michael Kurz, Erich Paulus
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Patent number: 6300371Abstract: A diterpene derivative compound, having the formula I, II, or III, compositions, and therapeutic compositions containing the compounds are disclosed. Also disclosed are methods for treating an inflammatory disorder by providing an inflammatory inhibiting amount of the compound as well as methods for obtaining the compound.Type: GrantFiled: April 16, 1999Date of Patent: October 9, 2001Assignees: Indian Institute of Chemical Technology, University of CaliforniaInventors: D. John Faulkner, Y. Venkateswarlu, K. V. Raghavan, J. S. Yadav
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Patent number: 6281198Abstract: Compound of formula (I): wherein: R represents: a group of formula (i): wherein X, Y and W are as defined in the description, or a group of formula (ii): —A—G (ii) wherein: A represents a single bond or an optionally substituted alkylene chain, G represents a group selected from hydrogen, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, —OR2, —O—T1—NR3R4, —O—T1—NR2—T′1—NR3R4, —NR3R4, —NR2—T1—NR3R4, —NR2—T1—OR5, —NR2—T1—CO2R6, —NR2—T1—C(O)R6, —C(O)—NR3R4, —C(O)—NR2—T2, —O—C(O)T2, —O—C(S)—T2, —NR2—C(O)—T2, —NR2—C(S)—T2, —O—C(O)—O—T2, —O—C(O)—NR2—T2, —O—C(S)—O—T2, —O—C(S)—NR2—T2, —NR2—C(O)—O—T2,Type: GrantFiled: October 26, 2000Date of Patent: August 28, 2001Assignee: Adir et CompagnieInventors: Claude Monneret, Emmanuel Bertounesque, Philippe Meresse, Ghanem Atassi, Alain Pierre, Bruno Pfeiffer, Pierre Renard
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Patent number: 6242617Abstract: Method of producing an antitumor preparation of natural origin lyophilized arglabin 1&bgr;, 10&bgr;-epoxy-13-dimethylamino-guaia-3(4)-en-6, 12-olide hydrochloride includes resin extraction from a natural material, its purification from worthless substances, resin separation into separate components by column chromatography with production of technical arglabin. Technical arglabin further undergoes recrystallization, amination and hydrochloration at given parameters of pH solutions with production of aminoarglabin hydrochloride and its further lyophilization and high quality identification by IR-spectroscopy. A device for the realization of the method is also disclosed herein.Type: GrantFiled: July 29, 1999Date of Patent: June 5, 2001Inventor: Sergazy Mynzhasarovich Adekenov
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Patent number: 6225339Abstract: This invention provides terpenoid lactone compounds, and processes for producing the terpenoid lactone compounds, which comprise cultivating Oidiodedron griseum FERM BP-5778 and then isolating the terpenoid lactone compounds from the fermentation broth. The present invention also provides a pharmaceutical composition comprising the terpenoid lactone compound, which is useful in the treatment of IL-1 and TNF mediated diseases or the like.Type: GrantFiled: January 15, 1999Date of Patent: May 1, 2001Assignee: Pfizer Inc.Inventors: Hiroyuki Nishida, Masaya Ikunaka, Nobuji Yoshikawa, Katsuomi Ichikawa, Nakao Kojima
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Patent number: 6207673Abstract: The present invention provides covalent conjugates of topoisomerase I and topoisomerase II inhibitors. Such compounds have a structure according to formula I: TI—L—TII (I) wherein: TI is a topoisomerase I inhibitor such as a camptothecin group; TII is a topoisomerase II inhibitor such as an amsacrine, ellipticine, epipodophyllotoxin, or anthracycline antibiotic group; and L is a linking group. The compounds are useful for inhibiting topoisomerase I and II enzymes, for promoting cellular differentiation, and for treating cancer.Type: GrantFiled: March 12, 1997Date of Patent: March 27, 2001Assignees: The University of North Carolina at Chapel Hill, Yale UniversityInventors: Kuo-Hsiung Lee, Yung-Chi Cheng, Xin Guo, Kenneth F. Bastow, Hui-Kang Wang
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Patent number: 6204257Abstract: The present invention is directed to novel water-soluble prodrugs of aliphatic or aromatic hindered hydroxyl group containing pharmaceuticals.Type: GrantFiled: August 7, 1998Date of Patent: March 20, 2001Assignee: Universtiy of KansasInventors: Valentino J. Stella, Jan J. Zygmunt, Ingrid Gunda Georg, Muhammad S. Safadi
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Patent number: 6197767Abstract: The invention provides various derivatives of arglabin, a sesquiterpene lactone isolated from Artemisia glabella. These compounds are effective for suppressing tumor growth in mammals. A method of suppressing tumor growth in humans is also described.Type: GrantFiled: October 7, 1998Date of Patent: March 6, 2001Assignee: Paracure, Inc.Inventor: Sergazy M. Adekenov
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Patent number: 6153645Abstract: Methods for treating infection and related compositions, compounds of formula I as defined in the application and methods for preparing same, are provided. In general, the compounds inhibit transfer ribonucleic acid (tRNA) synthetase and are useful as antimicrobial agents.Type: GrantFiled: September 10, 1999Date of Patent: November 28, 2000Assignee: Cubist Pharmaceuticals, Inc.Inventors: John Finn, Xiang Yang Yu, Zhongguo Wang, Jason Hill, Dennis Keith, Paul Gallant, Philip Wendler
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Patent number: 6083980Abstract: The compounds of Formula I ##STR1## are useful as immunosuppressive agents.Type: GrantFiled: October 1, 1998Date of Patent: July 4, 2000Assignee: Merck & Co., Inc.Inventors: Robert K. Baker, Jianming Bao, Frank Kayser, Shouwu Miao, William H. Parsons, Kathleen M. Rupprecht
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Patent number: 6051721Abstract: A process of preparing ring E-modified analogues of (-)-podophyllotoxin as potential new chemotherapeutic agents. The process generates corresponding analogues of (-)-podophyllotoxin, itself, and allows new molecular interactions in the southern hemisphere (ring E) of the molecule. A method of preparing enantiomerically enriched compounds of the formula (I) and (II): ##STR1## wherein R is: ##STR2## wherein X, X', Y, Y' and Z are ring E substituents and R.sup.1 is one of a)-e) below.a) --OH,b) an ether or glycoside,c) a substituted or unsubstituted amine or aniline,d) a C.sub.2 -C.sub.8 alkenyl group, preferably --CH.sub.2 CH.dbd.CH.sub.2,e) a C.sub.1 -C.sub.8 alcohol, preferably --CH.sub.2 CH.sub.2 CH.sub.2 OH.The process produces enantiomerically enriched compounds which do not occur naturally and are not readily available from (-)-podophyllotoxin.Type: GrantFiled: October 2, 1997Date of Patent: April 18, 2000Assignee: The Board of Regents of the University of NebraskaInventor: David Berkowitz
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Patent number: 6008382Abstract: A method for synthesizing a 4'-demethylepipodophyllotoxin of formula (II) from a podophyllotoxin of formula (I) by treating it with a pair of reagents, i.e. a strong acid and an aliphatic, aromatic or functionalized sulphide, in the present of an organic or inorganic acid, or in the presence of water with or without a water-miscible organic solvent.Type: GrantFiled: June 12, 1998Date of Patent: December 28, 1999Assignee: Pierre Fabre MedicamentInventors: Thierry Imbert, Yves Guminski
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Patent number: 5972998Abstract: The present invention relates to novel triptolide derivatives and a method of treating a patient suffering from an autoimmune disease comprising administering to a patient an effective amount of the novel triptolide derivatives.Type: GrantFiled: May 12, 1998Date of Patent: October 26, 1999Assignee: Hoechst Marion Roussel, Inc.Inventors: Michel J. Jung, Mahinda Wickramaratne, Michael Hepperle
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Patent number: 5965604Abstract: The present invention relates to chrolactomycin compound represented by the following formula (I): ##STR1## or pharmaceutically acceptable salts thereof having antibacterial and antitumor activities.Type: GrantFiled: December 17, 1998Date of Patent: October 12, 1999Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Yoshinori Yamashita, Ryuichiro Nakai, Tamio Mizukami, Shingo Kakita, Shigeru Chiba, Shiro Akinaga
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Patent number: 5902809Abstract: The invention provides various derivatives of arglabin, a sesquiterpene lactone isolated from Artemisia glabella. These compounds are effective for suppressing tumor growth in mammals. A method of suppressing tumor growth in humans is also described.Type: GrantFiled: September 19, 1997Date of Patent: May 11, 1999Assignee: Paracure, Inc.Inventor: Sergazy M. Adekenov
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Patent number: 5811034Abstract: Described are novel 7-methylidene-5-oxo-furo fused naphthopyran compounds having certain substituents at the 2 position of the pyran ring. Also described are polymeric organic host materials that contain or that are coated with such compounds.Type: GrantFiled: October 23, 1997Date of Patent: September 22, 1998Assignee: PPG Industries, Inc.Inventor: Jibing Lin
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Patent number: 5776962Abstract: Substituted lactone compounds are useful in the treatment of precancerous lesions and neoplasms.Type: GrantFiled: June 7, 1995Date of Patent: July 7, 1998Assignees: Cell Pathways, Inc., University of ArizonaInventors: Paul Gross, Gerhard Sperl, Rifat Pamukcu, Klaus Brendel
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Patent number: 5767042Abstract: Ring D-modified gibberellin compounds are effective in promoting or inducing a desired tissue morphology and/or physiological state in plants, giving effects such as growth retardation or inhibition and inhibition of floral development.Type: GrantFiled: May 8, 1997Date of Patent: June 16, 1998Assignees: The Australian National University, Commonwealth Scientific and Industrial Research Organization, Richard P. PharisInventors: Richard Persons Pharis, Lewis Norman Mander, Roderick Whitfield King
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Patent number: 5747520Abstract: Azatoxin and derivatives thereof are illustrative of a new class of antitumor drugs that are topoisomerase II (top 2) inhibitors. The pharmacophore inhibits the catalytic activity of the purified enzyme but does not unwind relaxed or supercoiled DNA. It is nonintercalative and has at least two domains: a quasi-planar polycyclic ring system, which may bind between DNA base pairs, and a pendant substituent thought to interact with the enzyme, with the DNA grooves or with both. In SV40 and c-myc DNA, azatoxin induces numerous double-strand breaks according to a cleavage pattern which differs from those of known top 2 inhibitors. Azatoxin also is a potent inhibitor of tubulin polymerization.Type: GrantFiled: June 2, 1995Date of Patent: May 5, 1998Inventors: Yves Pommier, Timothy Lee MacDonald, Jose S. Madalengoitia
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Patent number: 5580562Abstract: A Tripterygium wilfordii Hook F preparation having an improved LD.sub.50 in mice, an improved therapeutic activity:toxic index ratio and a lower amount of triptolide as compared to previous preparations is disclosed. The LD.sub.50 in mice of the T. wilfordii preparation is greater than about 860 mg/kg, the therapeutic activity:toxic index ratio is greater than about 2.6.times.10.sup.-3, and the amount of triptolide is less than about 1.3 .mu.g/mg. The preparation is useful for immunosuppression, in particular, the suppression of primary antibody response and suppression of autoimmune disease and for the treatment of rheumatoid arthritis.Type: GrantFiled: December 17, 1993Date of Patent: December 3, 1996Assignee: Board of Regents The University of Texas SystemInventors: Peter E. Lipsky, Xue L. Tao, Jian Cai
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Patent number: 5571914Abstract: A 4-desoxy-4-epipodophyllotoxin derivative of the following formula ##STR1## wherein R and R.sub.1 are as defined in the specification or a pharmaceutically acceptable salt thereof as well as an antitumor composition comprising such derivative or salt as an active ingredient.Type: GrantFiled: June 6, 1995Date of Patent: November 5, 1996Assignee: Taiho Pharmaceutical Co. Ltd.Inventors: Tadafumi Terada, Katsuhiko Fujimoto, Makoto Nomura, Junichi Yamashita, Setsuo Takeda, Takashi Kobunai, Hideo Yamaguchi, Konstanty Wierzba
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Patent number: 5547667Abstract: Conjugates of general formula 1:[A--O--W--Z].sub.a --T 1wherein the moiety A--O-- is the residue of drug of formula A--O--H in which --O--H is a primary or secondary hydroxyl group; a is an integer of from 1 to 30; W is a group of general formula 2: ##STR1## wherein b is an integer of from 1 to 4, B represents a C.sub.1 -C.sub.3 alkylene group and R.sub.1 and R.sub.2 each independently represent hydrogen, halogen, alkyl, phenyl or substituted phenyl; Z is a spacer group and T is a carrier moiety.Type: GrantFiled: October 25, 1994Date of Patent: August 20, 1996Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Francesco Angelucci, Laura Bersani, Michele Caruso, Marina Ripamonti, Daniela Ruggieri, Antonino Suarato
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Patent number: 5543429Abstract: There are disclosed novel compounds having the formula ##STR1## which exhibit antifungal activity.Type: GrantFiled: March 9, 1995Date of Patent: August 6, 1996Assignee: Merck & Co., Inc.Inventors: Gerald F. Bills, James E. Curotto, Sarah J. Dreikorn, Rosalind G. Jenkins, Jerrold M. Liesch, Sandra A. Morris, John R. Thompson, Deborah L. Zink, Richard K. Jansson, Angela Basilio, Teresa Diez, Fernando Pelaez, Francisca Vicente
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Patent number: 5541223Abstract: Novel podophyllotoxin compounds and their use in treating tumors are disclosed. The analogs have the general formula: ##STR1## wherein NH--R is a selected aryl amine, dialkylaminoalkyleneamino, or dialkylaminoanilino group.Type: GrantFiled: October 28, 1993Date of Patent: July 30, 1996Assignees: Yale University, The University of North Carolina at Chapel HillInventors: Kuo-Hsiung Lee, Yung-Chi Cheng