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| Number | Title | Issue Date |
| 8138343 | Crystalline polymorph of 7-ethyl-10-hydroxycamptothecin A crystalline polymorph of 7-ethyl-10-hydroxycamptothecin exhibiting an X-ray diffraction pattern having peaks at 10.9±0.2, 13.2±0.2, 23.9±0.2, and 26.1±0.2 2-theta degree. ... | 03/20/2012 |
| 8124769 | Stereoselective process and crystalline forms of a camptothecin A stereoselective process for preparing 7-[(E)-t-butyloxyiminomethyl]-camptothecin (also known as gimatecan) is herein disclosed. With the addition of further dissolution and precipitation steps carried out in appropriate different solvent mixtures, four new crystal... | 02/28/2012 |
| 8101758 | Stereoselective process and crystalline forms of a camptothecin A stereoselective process for preparing 7-[(E)-t-butyloxyiminomethyl]-camptothecin (also known as gimatecan) is herein disclosed. With the addition of further dissolution and precipitation steps carried out in appropriate different solvent mixtures, four new crystal... | 01/24/2012 |
| 8039626 | Method of manufacturing of 7-ethyl-10-hydroxycamptothecin The method of manufacturing of 7-ethyl-10-hydroxycamptothecin of formula I characterized in that 7-ethyl-1,2,6,7-tetrahydrocampotothecin of formula IV is oxidized with an oxidizing agent selected from the group comprising iodosobenzene, an ester of iodosobenzene, so... | 10/18/2011 |
| 8013158 | Crystalline forms of topotecan hydrochloride and processes for making the same Novel crystalline forms of topotecan hydrochloride and processes of making the same are disclosed. ... | 09/06/2011 |
| 8003795 | Compounds and compositions for reducing lipid levels Compositions comprising extracts or isolated or purified compounds from plants of the genus Corydalis provide prevention and treatment of hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, hepatic steatosis, and metabolic syndrome. Corydalis c... | 08/23/2011 |
| 7977483 | Process for making topotecan A process of making topotecan or a pharmaceutically acceptable salt thereof comprising reacting an iminium salt with 10-hydroxy-camptothecin. ... | 07/12/2011 |
| 7935822 | Carboxamide-substituted dyes for analytical applications The present invention relates to carboxamide-substituted dyes, the production and use of such dyes as labeling groups in analytics. ... | 05/03/2011 |
| 7928235 | Methods of making esters of camptothecins Methods of preparing CPT-esters are described. The methods include using at least one acid in the esterification reactions or acylation reactions of camptothecins. ... | 04/19/2011 |
| 7910737 | Process for the manufacturing of 7-ethyl-10-hydroxy camptothecin The invention discloses the preparation method of 7-ethyl-10-hydroxycamptothecin from 4-ethyl-7,8-dihydro-4-hydroxy-1H-pyrano[3,4-f]indolizine-3,6,10(4H)-trione and 1-(2-amino-5-hydroxyphenyl)-propan-1-one using higher reaction temperature and faster heating to that... | 03/22/2011 |
| 7799921 | Stereoselective process and crystalline forms of a camptothecin A stereoselective process for preparing 7-[(E)-t-butyloxyiminomethyl]-camptothecin (also known as gimatecan) is herein disclosed. With the addition of further dissolution and precipitation steps carried out in appropriate different solvent mixtures, four new crystal... | 09/21/2010 |
| 7781587 | Solubilized topoisomerase poisons 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. T... | 08/24/2010 |
| 7767813 | Preparation method The present invention is directed to a novel method for the preparation of high purity irinotecan. This can be achieved by eliminating the excess of the other reagent, bipiperidinyl-1′-carbonyl chloride after it has reacted with 7-ethyl-10-hydroxy camptothecin and... | 08/03/2010 |
| 7683170 | Methods for preparing Irinotecan Methods for manufacturing 7-ethyl-10-[4-(1-piperidino)-1-piperidino]-carbonyloxy-camptothecin are described comprising I. reacting a mixture of 1-chlorocarbonyl-4-piperidinopiperidine hydrochloride and 7-ethyl-10-hydroxycamptotheci... | 03/23/2010 |
| 7547785 | Process for preparing topotecan A process for preparing topotecan. ... | 06/16/2009 |
| 7544801 | Method of manufacturing of 7-ethyl-10-hydroxycamptothecin The method of manufacturing of 7-ethyl-10-hydroxycamptothecin of formula I characterized in that 7-ethyl-1,2,6,7-tetrahydrocampotothecin of formula IV is oxidized with an oxidizing agent selected from the group comprising iodosobenzene, an ester of iodosobenzene, so... | 06/09/2009 |
| 7507825 | Method of manufacturing of 7-ethyl-10-[4-(1-piperidino)-1- piperidino]- carbonyloxy- camptothecin The invention relates to the method of manufacturing of 7-ethyl-10-[4-(1-piperidino)-1-piperidino]-carbonyloxycamptothecin by condensation of 7-ethyl-10-hydroxycamptothecin with 1-chlorocarbonyl-4-piperidinopiperidine hydrochloride in a polar aprotic solvent in the ... | 03/24/2009 |
| 7495099 | High-molecular weight derivatives of camptothecins It is intended to provide water-soluble derivative of camptothecins which are excellent in therapeutic effect and suitable for chemotherapy for cancer. Namely, a water-soluble high-molecular weight derivative of camptothencins being excellent in sustained-release wh... | 02/24/2009 |
| 7488825 | Method for preparing polymorphism of irinotecan hydrochloride A method for preparing a novel crystalline polymorphic irinotecan hydrochloride which is excellent in the solubility in water and reduced in the content of impurities is provided. A method for preparing c-type crystals of irinotecan hydrochloride having diffraction ... | 02/10/2009 |
| 7435726 | Compositions and methods for the treatment of cancer This invention relates to compositions comprising thalidomide and another anti-cancer drug which can be used in the treatment or prevention of cancer. Preferred anti-cancer drugs are topoisomerase inhibitors. A particular composition comprises thalidomide, or a phar... | 10/14/2008 |
| 7435818 | Crystal forms of irinotecan hydrochloride The present invention provides for novel crystalline forms of irinotecan hydrochloride and processes for their preparation, pharmaceutical compositions containing the novel forms and methods for treating metastatic carcinoma of the colon or rectum using same. ... | 10/14/2008 |
| 7399860 | Manufacture of polyglutamate-therapeutic agent conjugates The invention provides new processes for preparing polyglutamic acid-therapeutic agent conjugates for clinical development and pharmaceutical use, and polyglutamic acid-therapeutic agent conjugates prepared by these processes. ... | 07/15/2008 |
| 7351830 | Pancratistatin cyclic phosphate prodrugs and phenpanstatin cyclic phosphate prodrugs Selective phosphorylation of phenpanstatin (3a) with tetrabutylammonium dihydrogen phosphate and dicyclohexyl-carbodiimide in pyridine followed by cation exchange chromatographic procedures was found to provide an efficient mute to a new series (3 | 04/01/2008 |
| 7351461 | Articles comprising benzopyran colorants, method of manufacture, and method of use An article comprising the compound of Formula (I) wherein X is hydrogen or a radical of Formula (II), R1 independently at each occurrence is a C1-C20 aliphatic radical, a C3-C | 04/01/2008 |
| 7351714 | 7-imino derivatives of camptothecin having antitumor activity 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 wit... | 04/01/2008 |
| 7323566 | Radiopharmaceutical and methods of synthesis and use thereof A novel group of apomorphine derivatives are provided that are well suited as radioimaging agents upon incorporation of radionuclides. Through reaction of D ring sites, the less reactive sites of the apomorphine A ring is modified in ways previously unattainable. | 01/29/2008 |
| 7319105 | Cytotoxic agents The invention provides compounds of the invention pharmaceutical compositions comprising a compound of the invention, processes for preparing compounds of the invention, intermediates useful for preparing compounds of the invention, and therapeutic methods for treat... | 01/15/2008 |
| 7312228 | Cytotoxic indeno and isoindoloisoquinolones The synthesis and biological activity of benzoisoindoloisoquinolone compounds are described. The synthesis and biological activity of C-11-substituted indenoisoquinolones are also described. Indenoisoquinolones substituted at C-11 are prepared by McMurry reactions o... | 12/25/2007 |
| 7301025 | Colorant compounds Compounds of the formula wherein M is either (1) a metal ion having a positive charge of +p wherein p is an integer which is at least 2, said metal ion being capable of forming a compound with at least two chromo... | 11/27/2007 |
| 7273627 | Botanical compositions having hypoglycemic, hypolipidemic and antimicrobial activities for maintaining good health in normal person and diabetic patient Botanical compositions are described having hypoglycemic, hypolipidemic and antimicrobial activity for maintaining good health in normal person and diabetic person comprising water extract of two medicinal plants, dried leaves of Malvastrum coromandelianum an... | 09/25/2007 |
| 7273873 | Camptothecins with a modified lactone ring Compounds of formula (I) or (II) are described: where the groups are as defined in the description here below, the racemic mixtures, their individual enantiomers, their individual diastereoisomers, their mixtures, and their pharmaceutically acceptable salts. Said co... | 09/25/2007 |
| 7270772 | Benzopyran colorants, method of manufacture, and method of use A compound of Formula (I) wherein X is hydrogen or a radical of Formula (II), R1 independently at each occurrence is a C1–C20 aliphatic radical, a C3–C10 | 09/18/2007 |
| RE39707 | Camptothecin derivatives (20S) esters of camptothecin analogs are provided. The compounds are (20S) esters of an oxyalkanoic acid and camptothecin, which is are optionally substituted at the 7, 9, 10, 11, and 12 positions of the camptothecin ring. The compounds are useful for treating canc... | 06/26/2007 |
| 7223770 | Tocopherol-modified therapeutic drug compounds Tocopherol-modified therapeutic drug compounds; emulsion, microemulsion, and micelle formulations that include the compounds; methods for making the compounds and formulations; methods for administering the compounds and formulations; and methods for treating condit... | 05/29/2007 |
| 7214710 | Permeable, water soluble, non-irritating prodrugs of chemotherapeutic agents with oxaalkanoic acids The present invention relates to the field of prodrugs of chemotherapeutic agents and method of use thereof. ... | 05/08/2007 |
| 7208492 | Topoisomerase-targeting agents The invention provides compounds of formula I or formula II: wherein: the bond represented by --- is a single bond or a double bond, and R1–R5, X, and Y have any of the meanin... | 04/24/2007 |
| 7176317 | Colorant compounds Compounds of the formula wherein R1, R2, R3, R4, R5, R6, R7, a, b, c, d, Y, Q, Q—, A, and CA are as defined herein. ... | 02/13/2007 |
| 7169922 | Derivatives of 1,2-dihydro-7-hydroxyquinolines containing fused rings The present invention describes novel dyes, including coumarins, rhodamines, and rhodols that incorporate additional fused aromatic rings. The dyes of the invention absorb at a longer wavelength than structurally similar dyes that do not possess the fused aromatic r... | 01/30/2007 |
| 7153946 | Molecular conjugates for use in treatment of cancer A molecular conjugate is provided having the formula: wherein R1 is a de-hydroxyl or de-amino moiety respectively of a hydroxyl-bearing or amino-bearing biologically active molecule or an analog or der... | 12/26/2006 |
| 7151179 | Process for the preparation of 7-alkyl-10-hydroxy-20(S)-camptothecin The key intermediate in any synthesis of Irinotecan is 7-ethyl-10-hydroxy-20(S)-camptothecin. A process for the efficient synthesis of this intermediate is demonstrated proceeding through readily available 20(S)-camptothecin. Various other tecan compounds may be mad... | 12/19/2006 |
