Three Or More Ring Hetero Atoms In The Pentacyclo Ring System Patents (Class 546/48)
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Patent number: 7030243Abstract: A process for synthesizing highly lipophilic derivatives of camptothecin. The process includes reacting dissolved, underivatized camptothecin with a silylated heterocyclic compound in a modified Minisci-type alkylation reaction to produce 7-substituted derivatives of camptothecin.Type: GrantFiled: October 28, 2004Date of Patent: April 18, 2006Assignee: BioNumerik Pharmaceuticals, Inc.Inventors: Ye Wu, Kesavaram Narkunan, Jianyan Wang, Harry Kochat
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Patent number: 7012079Abstract: The invention relates in particular to the compounds of general formula in which R1, R2, R3, R4, R5, R6 represent various radicals; their use as medicaments and pharmaceutical compositions containing them. These compounds are particularly useful for the treatment of cancer.Type: GrantFiled: February 24, 2000Date of Patent: March 14, 2006Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)Inventors: Olivier Lavergne, Dennis Bigg, Christophe Lanco, Alain Rolland
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Patent number: 6992089Abstract: The invention provides compounds of formula I: wherein R1-R9, W, and X have any of the meanings defined in the specification and their pharmaceutically acceptable salts. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I, and therapeutic methods for treating cancer and infections using compounds of formula I.Type: GrantFiled: August 11, 2003Date of Patent: January 31, 2006Assignee: Rutgers, The University of New JerseyInventors: Edmond J. LaVoie, Alexander L. Ruchelman, Leroy F. Liu
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Patent number: 6992088Abstract: The invention provides compounds of formula I: wherein: R1-R5, “a” and X have any of the meanings defined in the specification and their pharmaceutically acceptable salts. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I, and therapeutic methods for treating cancer using compounds of formula I.Type: GrantFiled: August 11, 2003Date of Patent: January 31, 2006Assignee: Rutgers, The State University of New JerseyInventors: Edmond J. LaVoie, Sudhir K. Singh, Leroy F. Liu
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Patent number: 6989387Abstract: The invention provides compounds of formula I: wherein R1–R9, W, and X have any of the meanings defined in the specification and their pharmaceutically acceptable salts. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I, and therapeutic methods for treating cancer using compounds of formula I.Type: GrantFiled: August 11, 2003Date of Patent: January 24, 2006Assignee: Rutgers, The State University of New JerseyInventors: Edmond J. LaVoie, Sudhir K. Singh, Leroy F. Liu
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Patent number: 6987109Abstract: The invention provides compounds of formula I: wherein A, B, W, Y, Z, and R1 have any of the meanings defined in the specification and their pharmaceutically acceptable salts. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I, and therapeutic methods for treating cancer using compounds of formula I.Type: GrantFiled: May 14, 2004Date of Patent: January 17, 2006Assignee: Rutgers, The State University of New JerseyInventors: Edmond J. LaVoie, Alexander L. Ruchelman
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Patent number: 6982333Abstract: The present invention provides a short, convergent total synthesis of camptothecin and related compounds which consists of a novel 4+1 radical annulation. The present invention also provides novel chemical intermediates for such 4+1 radical annulations.Type: GrantFiled: September 16, 2003Date of Patent: January 3, 2006Assignee: University of PittsburghInventors: Dennis P. Curran, Hubert Josien, Sung Bo Ko
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Patent number: 6967215Abstract: Tetrahydrocarbazoles of formula where Q is —SO2—; —O—; or —(CO)—; X is —(CH)—; or —N—; m is from 1 to 3; t is 0 or 1 and the remaining substituents are as defined herein, are useful as antimicrobial active ingredients.Type: GrantFiled: September 11, 2001Date of Patent: November 22, 2005Assignee: Ciba Specialty Chemicals CorporationInventors: Wolfgang Haap, Andreas Mehlin, Karin Petzold, Dietmar Ochs, Werner Hölzl
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Patent number: 6964964Abstract: The invention provides compounds of formula I: wherein A, B, W, Y, Z, R1, R3 and R4 have any of the meanings defined in the specification and their pharmaceutically acceptable salts. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I, and therapeutic methods for treating cancer using compounds of formula I.Type: GrantFiled: May 14, 2004Date of Patent: November 15, 2005Assignee: Rutgers The State University of New JerseyInventors: Edmond J. LaVoie, Alexander L. Ruchelman
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Patent number: 6933302Abstract: (20) esters of camptothecin analogs are provided. The compounds are (20) esters of an aminoalkanoic acid or an imidoalkanoic acid and homocamptothecin, which is optionally substituted at the 7, 9, 10, 11, and 12 positions of the homocamptothecin ring. The compounds are useful for treating cancer.Type: GrantFiled: June 3, 2003Date of Patent: August 23, 2005Assignees: California Pacific Medical Center, Catholic Healthcare WestInventor: Li-Xi Yang
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Patent number: 6916800Abstract: The present invention provides methods to treat or prevent neoplasia disorders in a mammal using a combination of a matrix metalloproteinase inhibitor and an antineoplastic agent.Type: GrantFiled: September 20, 2004Date of Patent: July 12, 2005Assignee: Pfizer IncInventors: John P. McKearn, Gary Gordon, James J. Cunningham, Stephen T. Gately, Alane T. Koki, Jaime L. Masferrer
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Patent number: 6897200Abstract: Camptothecin drugs are stabilized in their antitumor active lactone form by complexation with an oligonucleotide including RNA or catalytic RNA. The oligonucleotide-camptothecin drug complex may be incorporated within a macromolecular assembly including both viral and non-viral oligonucleotide vectors. The invention allows combination gene and camptothecin drug therapy.Type: GrantFiled: October 14, 1998Date of Patent: May 24, 2005Assignee: University of Kentucky Research FoundationInventors: Thomas G. Burke, Ayhan S. Demir, Ashok J. Chavan, Danzhou Yang
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Patent number: 6893668Abstract: The present invention relates to an improved and economical process for the isolation of anticancer agent Camptothecin from the twigs and stem of Nothapodytes foetida using hot extraction 20(S) Camptothecin is an alkaloid, which contains a pentacyclic ring system that includes a pyrrolo [3,4-b] quinoline moiety (ring A, B and C), the pyridone ring D and a chiral center at C-20 in ring E.Type: GrantFiled: March 31, 2003Date of Patent: May 17, 2005Assignee: Council of Scientific and Industrial ResearchInventors: Santosh Kumar Srivastava, Merajuddin Khan, Suman Preet Singh Khanuja
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Patent number: 6872829Abstract: A convenient and efficient process for direct preparation of 5-alkoxy and 5-acyloxy analogues of camptothecins (anticancer compounds) and mappicine ketones (antiviral compounds) has been invented by treatment of the parent compounds with alcohols and acids respectively in the presence of ceric ammonium nitrate (CAN) at room temperature. The process is simple, economic and completed within a short period of time.Type: GrantFiled: December 30, 2002Date of Patent: March 29, 2005Assignee: Council of Scientific and Industrial ResearchInventors: Biswanath Das, Purushotham Madhusuda, Venkata Naga Satya Srinivas Kalavagunta
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Patent number: 6858598Abstract: A method of using an MMP inhibitor and optionally radiation therapy, and one or more antineoplastic agents of the topoisomerase class selected from the group consisting of irinotecan and topotecan, as a combination therapy for the treatment of neoplasia is disclosed.Type: GrantFiled: December 22, 1999Date of Patent: February 22, 2005Assignee: G. D. Searle & Co.Inventors: John P. McKearn, Gary Gordon, James J. Cunningham, Stephen T. Gately, Alane T. Koki, Jaime L. Masferrer
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Patent number: 6855720Abstract: (20S) esters of camptothecin analogs are provided. The compounds are (20S) esters of an aminoalkanoic acid or an imidoalkanoic acid and camptothecin, which is optionally substituted at the 7, 9, 10, 11, and 12 positions of the camptothecin ring. The compounds are useful for treating cancer.Type: GrantFiled: June 14, 2002Date of Patent: February 15, 2005Assignees: California Pacific Medical Center, Catholic Healthcare WestInventor: Li-Xi Yang
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Publication number: 20040266804Abstract: Camptothecin analogs having an E-ring ketone are effective anti tumor compounds. These compounds inhibit the enzyme topoisomerase I and may alkylate DNA of the associated topoisomerase I DNA cleavable complex.Type: ApplicationFiled: June 30, 2003Publication date: December 30, 2004Applicant: Research Triangle InstituteInventors: Monroe E. Wall, Mansukh C. Wani, Govindarajan Manikumar, Michael A. Wall
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Publication number: 20040266803Abstract: Methods of forming camptothecin compounds which are effective anti-tumor compounds are disclosed. These compounds inhibit the enzyme topoisomerase I and may alkylate DNA of the associated topoisomerase I-DNA cleavable complex.Type: ApplicationFiled: June 27, 2003Publication date: December 30, 2004Applicant: Research Triangle InsituteInventors: Mansukh C. Wani, Govindarajan Manikumar, Monroe E. Wall, Michael A. Wall
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Patent number: 6825207Abstract: (20S) esters of camptothecin analogs are provided. The compounds are (20S) esters of an aminoalkanoic acid or an imidoalkanoic acid and camptothecin, which is optionally substituted at the 7, 9, 10, 11, and 12 positions of the camptothecin ring. The compounds are useful for treating cancer.Type: GrantFiled: May 23, 2002Date of Patent: November 30, 2004Assignees: California Pacific Medical Center, Catholic Healthcare WestInventors: Li-Xi Yang, Xiandao Pan, Huijuan Wang
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Patent number: 6825166Abstract: A molecular conjugate is provided having the formula: wherein n is the conjugation number, P is a moiety of a carrier molecule such as a protein, R1 is a moiety of a biologically active molecule or its analogs, derivatives, salts or secondary amines, Z is —O— or —NH—, and Y is a straight or branched alkyl having 1 to 20 carbons optionally substituted with one or more phenyl, a cycloalkyl optionally substituted with one or more alkyl or phenyl, or an aromatic group optionally substituted with one or more alkyl, electron-withdrawing or electron-donating groups. Compounds and methods useful in producing such molecular conjugates are also provided, as well as methods of concentrating biologically active molecules in selected target cells of a patient that comprise administering to the patient a selected dose of such molecular conjugates.Type: GrantFiled: March 25, 2002Date of Patent: November 30, 2004Assignee: Tapestry Pharmaceuticals, Inc.Inventors: James D. McChesney, Madhavi C. Chander, Teruna J. Siahaan, Christine R. Xu, Sterling K. Ainsworth
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Patent number: 6815546Abstract: A compound of the formula wherein the substituents are defined as in the specification which compounds are useful in the treatment of cancer.Type: GrantFiled: February 6, 2002Date of Patent: November 9, 2004Assignee: Societe de Recherches et d'Applications Scientifiques (S.C.R.A.S.)Inventors: Dennis Bigg, Olivier Lavergne, Francesc Pla Rodas, Jacques Pommier, Gérard Ulibarri, Jerry Harnett, Alain Rolland, Anne-Marie Liberatore, Christophe Lanco, Jean-Bernard Cazaux, Christine Le Breton, Eric Manginot
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Patent number: 6765019Abstract: The present invention relates to the field of prodrugs of chemotherapeutic agents and method of use thereof.Type: GrantFiled: May 4, 2000Date of Patent: July 20, 2004Assignee: University of Kentucky Research FoundationInventors: Peter A. Crooks, Tadeusz Cynkowski, Grazyna Cynkowska, Hong Guo, Paul Ashton
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Patent number: 6762301Abstract: A process for the preparation of a compound of the formula wherein the substituents are defined as set forth in the specification comprising reacting a compound of the formula with a 2-halo-3-quinoline-methanol of the formula to obtain a compound of the formula which is then cyclized to form the compound of Formula I.Type: GrantFiled: January 30, 2002Date of Patent: July 13, 2004Assignee: Societe de Conseils de Recherches et Applications Scientifiques (S.C.R.A.S.)Inventors: Dennis Bigg, Olivier Lavergne, Francesc Pla Rodas, Jacques Pommier, Gerard Ulibarri, Jerry Harnett, Alain Rolland, Anne-Marie Liberatore, Christophe Lanco, Jean-Bernard Cazaux, Christine Le Breton, Eric Manginot
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Patent number: 6759416Abstract: The present invention provides novel conjugates of camptothecin compounds and long-chain unsaturated fatty acid. The novel conjugates can be used to treat mammalian cell proliferative diseases such as cancer.Type: GrantFiled: June 9, 2003Date of Patent: July 6, 2004Assignee: Panorama Research, Inc.Inventor: Yuqiang Wang
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Publication number: 20040127711Abstract: A convenient and efficient process for direct preparation of 5-alkoxy and 5-acyloxy analogues of camptothecins (anticancer compounds) and mappicine ketones (antiviral compounds) has been invented by treatment of the parent compounds with alcohols and acids respectively in the presence of ceric ammonium nitrate (CAN) at room temperature. The process is simple, economic and completed within a short period of time.Type: ApplicationFiled: December 30, 2002Publication date: July 1, 2004Applicant: Council of Scientific and Industrial ResearchInventors: Biswanath Das, Madhusudhan Purushotham, Venkata Naga Satya Sriniva Kalavagunta
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Publication number: 20040110782Abstract: The invention provides compounds of formula I: 1Type: ApplicationFiled: August 11, 2003Publication date: June 10, 2004Inventors: Edmond J. LaVoie, Sudhir K. Singh, Leroy F. Liu
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Publication number: 20040110760Abstract: The invention provides compounds of formula I: 1Type: ApplicationFiled: August 11, 2003Publication date: June 10, 2004Inventors: Edmond J. LaVoie, Sudhir K. Singh, Leroy F. Liu
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Patent number: 6743918Abstract: Problem: A large scale production of camptothecin, which is a starting compound of irinotecan hydrochloride and various camptothecin derivatives, at a low cost and with ease. Solution: A process for preparing camptothecin, characterized in that it comprises the following steps (a) and (b); (a) the step to hydrolyze 9-methoxycamptothecin or a natural material containing 9-methoxycamptothecin; (b) the step to convert 9-hydroxycamptothecin obtained in the step (a) into camptothecin by 9-O—perfluoro-lower-alkylsulfonylation or 9-O—phenyltetrazolylation, followed by hydrogenolysis.Type: GrantFiled: November 25, 2002Date of Patent: June 1, 2004Assignee: Kabushiki Kaisha Yakult HonshaInventors: Takashi Yaegashi, Takanori Ogawa, Seigo Sawada
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Patent number: 6737280Abstract: A class of asymmetric monobenzoxanthene compounds useful as fluorescent dyes are disclosed having structure (I) wherein Y1 and Y2 are individually hydroxyl, amino, imminium, or oxygen, R1-R8 are hydrogen, fluorine, chlorine, alkyl, alkene, alkyne, sulfonate, amino, amido, nitrile, alkoxy, linking group, and combinatios thereof, and R9 is acetylene, alkane, alkene, cyano, substituted phenyl, and combinations thereof. The invention further includes novel intermediate compounds useful for the synthesis of asymmetric benzoxanthene compounds having general structure (II) where substituents R3-R7 correspond to like-referenced substituents in the structure of described above, and Y2 is hydroxyl or amine. In another aspect, the invention includes methods for synthesizing the above dye compounds and intermediates. In yet another aspect, the present invention includes reagents labeled with the asymmetric benzoxanthene dye compounds, including deoxynucleotides, dideoxynucleotides, phosphoramidites, and polynucleotides.Type: GrantFiled: November 26, 2001Date of Patent: May 18, 2004Assignee: Karl-Heinz DrexhageInventors: Karl-Heinz Drexhage, Jutta Arden-Jacob, Norbert Kemnitzer
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Publication number: 20040077672Abstract: A compound selected from those of formula (I): 1Type: ApplicationFiled: September 26, 2003Publication date: April 22, 2004Inventors: Michelle Prudhomme, Bernadette Hugon, Fabrice Anizon, John Hickman, Alain Pierre, Roy Golsteyn, Pierre Renard, Bruno Pfeiffer
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Patent number: 6723729Abstract: Novel compounds are provided having the formula and salt thereof, where R1 is hydrogen, an alkyl, aralkyl, hydroxymethyl, carboxymethyl acyloxymethyl or trialkylsilyl group, or a group —CH2NR3R4 where N is a linking nitrogen atom and where (a) R3 and R4 are independently selected from hydrogen and alkyl, alkenyl, hydroxyalkyl and alkoxyalkyl groups; (b) R3 is hydrogen or an alkyl, alkenyl, hydroxyalkyl or alkoxyalkyl group, and R4 is —COR5 where R5 is hydrogen or an alkyl, alkenyl, hydroxyalkyl or alkoxyalkyl group; or (c) R3 and R4 taken together with the linking nitrogen atom form a saturated 3- to 7-member heterocyclic group. These compounds are useful intermediates in a process to prepare camptothecin derivatives including the anti-cancer drug irinotecan.Type: GrantFiled: April 16, 2003Date of Patent: April 20, 2004Assignee: Pharmacia and Upjohn CompanyInventor: Kevin E. Henegar
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Patent number: 6723849Abstract: A process for synthesizing highly lipophilic derivatives of camptothecin. The process includes reacting dissolved, underivatized camptothecin with an aldehyde in a modified Minisci-type alkylation reaction to produce 7-substituted derivatives of camptothecin.Type: GrantFiled: July 25, 2003Date of Patent: April 20, 2004Assignee: BioNumerik Pharmaceuticals, Inc.Inventors: Kesavaram Narkunan, Harry Kochat, Xinghai Chen
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Patent number: 6716982Abstract: The present invention relates to a process for preparing camptothecin and camptothecin analogs of Formula (I) from compounds of Formula (II) and to novel intermediates useful in their preparation, wherein R1 to R6 represent various substituents.Type: GrantFiled: July 11, 2001Date of Patent: April 6, 2004Assignee: OSI Pharmaceuticals, Inc.Inventors: Francis Gerard Fang, Shiping Xie
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Publication number: 20040063740Abstract: (20) esters of camptothecin analogs are provided. The compounds are (20) esters of an aminoalkanoic acid or an imidoalkanoic acid and homocamptothecin, which is optionally substituted at the 7, 9, 10, 11, and 12 positions of the homocamptothecin ring. The compounds are useful for treating cancer.Type: ApplicationFiled: June 3, 2003Publication date: April 1, 2004Inventor: Li-Xi Yang
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Publication number: 20040063947Abstract: The present invention provides a short, convergent total synthesis of camptothecin and related compounds which consists of a novel 4+1 radical annulation. The present invention also provides novel chemical intermediates for such 4+1 radical annulations.Type: ApplicationFiled: September 16, 2003Publication date: April 1, 2004Inventors: Dennis P. Curran, Hubert Josien, Sung Bo Ko
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Patent number: 6703399Abstract: Halo-alkyl esters of camptothecin are described. Processes for making these compounds and for using them in cancer treatment, are also described.Type: GrantFiled: May 6, 2002Date of Patent: March 9, 2004Assignee: The Stehlin Foundation for Cancer ResearchInventors: Zhisong Cao, Beppino C. Giovanella
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Patent number: 6699875Abstract: Cascade esters of camptothecin are described. Processes for making these compounds and for using them in cancer treatment are also described.Type: GrantFiled: May 6, 2002Date of Patent: March 2, 2004Assignee: The Stehlin Foundation for Cancer ResearchInventors: Zhisong Cao, Beppino C. Giovanella
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Patent number: 6696458Abstract: Amorphous forms of 9-nitrocamptothecin are provided by grinding or pulverizing different polymorphic forms of 9-nitrocamptothecin, and the polymorphic forms are characterizable as having an X-ray powder diffraction pattern with discernable diffraction lines at different °2&thgr; values for Cu K&agr; radiation having a wavelength of 1.5406 Angstrom.Type: GrantFiled: October 8, 2002Date of Patent: February 24, 2004Assignee: Super Gen, Inc.Inventors: Sanjeev Redkar, Ashok Gore
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Publication number: 20040034050Abstract: C-20 esters of homo-camptothecin analogues are provided. The compounds are C-20 esters of an oxyalkanoic acid and homo-camptothecin, which are optionally substituted at the 7, 9, 10, 11, and 12 positions of the homo-camptothecin ring. The compounds are useful for treating cancer.Type: ApplicationFiled: June 3, 2003Publication date: February 19, 2004Inventor: Li-Xi Yang
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Patent number: 6660861Abstract: The present invention relates to the use of dihalomethanes as reagents for the preparation of Topotecan{4-(S)-10(dimethylamino)-methyl-4-ethyl 4,9 dihydroxyl-H-pyrano[3′4′:6,7]indolizino-[1,2-b]quinoline-3,14(4H,12H)dione} from 10-hydroxycamptothecin. The invention discloses the rationale use of dichloromethane under solid-liquid phase transfer catalysis, which can behave both as solvent and a reactant when it serves as a source for C-1 unit for amino-alkylation of 10-hydroxy-4-(S)camptothecin.Type: GrantFiled: March 27, 2003Date of Patent: December 9, 2003Assignee: Council of Scientific and Industrial ResearchInventors: Satish Chander Puri, Geeta Handa, Kanaya Lal Dhar, Om Parkash Suri, Ghulam Nabi Qazi
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Patent number: 6656948Abstract: Compounds of the following formula: wherein all variables are as defined in the specification. The compounds have cytotoxic properties and can therefore be used in the treatment of malignant tumors.Type: GrantFiled: September 24, 2001Date of Patent: December 2, 2003Assignee: Universidad Complutense de MadridInventors: José Luis Fernandez Puentes, Dolores Garcia Gravalos, Carmen Avendano Lopez, Maria del Mar Blanco Castro, Jose Carlos Menendez Ramos
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Patent number: 6653319Abstract: The present invention provides a general method to retard the precipitation inception time for poorly water-soluble camptothecin analogues from a supersaturated solution by a chemical conversion approach via pH alteration. This method is successfully utilized to prepare stable parenteral formulations for silatecan 7-t-butyldimethylsilyl-10-hydroxycamptothecin (DB-67), a poorly water-soluble lipophilic camptothecin analogue, in aqueous solutions containing &bgr;-cyclodextrin sulfobutyl ether (SBE-CD) or other solubilizing agents. The formulations manufactured by this method are more simple and cost-effective, of higher doses and better quality in terms of manufacture loss and formulation stability, and can be free of organic solvents (e.g., DMSO or N-methyl-2-pyrrolidinone).Type: GrantFiled: August 12, 2002Date of Patent: November 25, 2003Assignee: University of Kentucky Research FoundationInventors: Tian-Xiang Xiang, Bradley D. Anderson
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Patent number: 6645975Abstract: The present invention relates to a novel process for the preparation of compounds of the formula wherein R1, R2, R4, R5, R6 and A are as defined herein, and to certain derivations of Formula IX which are useful for the treatment of movement disorders.Type: GrantFiled: January 27, 2003Date of Patent: November 11, 2003Assignee: Purdue Research FoundationInventors: Sing-Yuen Sit, Swanee E. Jacutin-Porte
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Patent number: 6620937Abstract: The present invention provides a short, convergent total synthesis of camptothecin and related compounds which consists of a novel 4+1 radical annulation. The present invention also provides novel chemical intermediates for such 4+1 radical annulations.Type: GrantFiled: March 23, 2001Date of Patent: September 16, 2003Assignee: University of PittsburghInventors: Dennis P. Curran, Hubert Josien, Sung Bo Ko
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Patent number: 6617456Abstract: A camptothecin derivative comprising a compound of the formula [I]: wherein R1, R2, R3, R4 and R5 are (A) adjacent two groups combine to form alkylene, or both are H, and one of the remaining three groups is —Xn-Alkm-R6, and the other two are H, alkyl or halogen, or (B) adjacent two groups combine to form alkylene, and one of the carbon atoms of said alkylene group is substituted by —Xn-Alkm-R6, and the remaining three groups are H, alkyl or a halogen, and one or two —CH2— of the alkylene in (A) or (B) may optionally be replaced by —O—, —S— or —NH—, X is —O— or —NH—, Alk is alkylene, or —OH, m and n are both 0 or 1, or m is 1 and n is 0, which camptothecin compound is bound to a polysaccharide having carboxyl groups via an amino acid or a peptide, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: July 21, 2000Date of Patent: September 9, 2003Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Kenji Tsujihara, Takayuki Kawaguchi, Satoshi Okuno, Toshiro Yano
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Patent number: 6608052Abstract: Disclosed are novel aromatic compounds of the formula(I) wherein G, E, W, Ar, X, Y and Z. The compounds are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are pharmaceutical compositions containing and processes of making such compounds.Type: GrantFiled: April 13, 2001Date of Patent: August 19, 2003Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Steffen Breitfelder, Pier F. Cirillo, John R. Regan
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Patent number: 6593334Abstract: Compounds according to formula I: C′—L—T (I), wherein C′ is a camptothecin group; L is a linking moiety; T is a taxoid group, pharmaceutically acceptable salt thereof. The compounds are useful in, among other things, treating cancer in subjects in need thereof, including cellular differentiation, and inhibiting cellular mitosis.Type: GrantFiled: May 2, 2002Date of Patent: July 15, 2003Assignee: The University of North Carolina at Chapel HillInventors: Kuo-Hsiung Lee, Hironari Ohtsu, Yuka Nakanishi, Kenneth F. Bastow, Fang-Yu Lee
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Patent number: 6589939Abstract: Camptothecin derivatives of camptothecin of formula (I): wherein the groups R1, R2 and R3 are as defined in the description are disclosed. The compounds of formula (I) are endowed with antitumor activity and show a good therapeutic index. Processes for the preparation of the compounds of formula (I) and their use in the preparation of medicaments useful in the treatment of tumors, viral infections and antiplasmodium falciparum are also disclosed.Type: GrantFiled: December 22, 2000Date of Patent: July 8, 2003Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Sergio Penco, Lucio Merlini, Paolo Carminati, Franco Zunino
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Patent number: 6583150Abstract: A pharmaceutical composition comprising an efficient amount of a compound selected among the compounds of formulae (I) and (II). The compounds have useful cytotoxic properties providing therapeutic application as antitumoral medicine.Type: GrantFiled: September 18, 2001Date of Patent: June 24, 2003Assignee: Laboratorie L. LafonInventors: Evelyne Delfourne, Nathalie Bontemps-Subielos, Francis Darro, Jean Bastide, Robert Kiss, Armand Frydman
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Patent number: RE38408Abstract: A method is disclosed for the preparation of 9-nitrocamptothecin which involves reacting 20-camptothecin with at least one inorganic nitrate salt and at least one acid effective in catalyzing the formation of a nitronium ion, where the reaction occurs at a temperature and for a time sufficient to form the 9-nitrocamptothecin. Also, methods of further purifying the 9-nitrocamptothecin by column chromatography or by reprecipitation is also disclosed.Type: GrantFiled: June 9, 2000Date of Patent: January 27, 2004Assignee: The Stehlin Foundation for Cancer ResearchInventor: Zhisong Cao