|
Match
|
Document |
Document Title |
|
|
7612081 |
7-Polyaminoalkyl(oxy)iminomethylcamptothecins bearing protective groups
Compounds are disclosed with the general formula
in which the groups are as defined in the description here below and characterized by the presence of polyamine substituents on the imine/oxime...
|
|
|
7608740 |
Method of synthesizing key intermediates for the production of camptothecin derivatives
The present invention discloses a process for efficient production of 2-amino-5-hydroxypropiophenone corresponding to the AB ring part of camptothecin (CPT) skeleton, which is a key intermediate...
|
|
|
7601733 |
5(S)-(2′-hydroxyethoxy)-20(S)-camptothecin and its preparation and use for the treatment of cancer
A 5(S)-(2′-hydroxyethoxy)-20(S)-camptothecin diasterisomer is described which is a better inhibitor of topoisomerase I than either the diastereoisomeric mixture...
|
|
|
7601732 |
Crystalline form of 5(S)-(2-hydroxyethoxy)-20(S)-camptothecin
A crystalline form of 5(S)-(2′-hydroxyethoxy)-20(S)-camptothecin diastereoisomer of 5(RS)-(2′-hydroxyethoxy)-20(S)-camptothecin is described that is characterized by having an X-ray powder...
|
|
|
7589099 |
7-t-butoxyiminomethylcamptothecin conjugated in position 20 with integrin antagonists
Compounds of Formula (I) are described:
in which the R 1 group is as defined in the specification and includes the condensation of 7-t-butoxyiminomethylcamptothecin in position 20 with a...
|
|
|
7572803 |
Hydrated crystalline esters of camptothecin
Hydrated crystalline camptothecin esters, such as crystalline aliphatic ester hydrates of camptothecin, pharmaceutical compositions containing crystalline aliphatic ester hydrates of camptothecin,...
|
|
|
7547785 |
Process for preparing topotecan
A process for preparing topotecan.
|
|
|
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...
|
|
|
7531550 |
Pseudobase benzo[c]phenanthridines with improved efficacy, stability, and safety
Pseudobase benzo[c]phenanthridines and the pharmaceutically acceptable salts thereof of Formula I
are provided herein. The variables R, R 1 , R 2 , R 3 , and R 4 are defined herein. Certain...
|
|
|
7517883 |
Solubilized topoisomerase poisons
The invention provides compounds of formula I:
wherein
A, B, W, Y, Z, and R 1 have any of the meanings defined in the specification and their pharmaceutically acceptable salts. The invention...
|
|
|
7517867 |
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 R 1 -R 5 , X, and Y have any of the meanings defined...
|
|
|
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]-carbonyloxycampto
thecin by condensation of 7-ethyl-10-hydroxycamptothecin with...
|
|
|
7498340 |
Esters in position 20 of camptothecins
Formula (I) compounds are described: (I) where the groups are as defined in the description here below, the racemic mixtures, their individual enantiomers, their individual diastereoisomers, their...
|
|
|
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...
|
|
|
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...
|
|
|
7462627 |
Multi-arm polymeric conjugates of 7-ethyl-10-hydroxycamptothecin for treatment of breast, colorectal, pancreatic, ovarian and lung cancers
A four arm-polyethylene glycol-7-ethyl-10-hydroxycamptothecin conjugate, such as,
is disclosed. Methods of making the conjugates and methods of treating mammals using the same are also disclosed.
|
|
|
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...
|
|
|
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...
|
|
|
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...
|
|
|
7351714 |
7-imino derivatives of camptothecin having antitumor activity
Camptothecin derivatives of camptothecin of formula (I)
wherein the groups R 1 , R 2 and R 3 are as defined in the description are disclosed.
The compounds of formula (I) are endowed with...
|
|
|
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), R 1 independently at each occurrence is a C 1 -C 20 aliphatic radical, a C 3 -C 10 ...
|
|
|
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...
|
|
|
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...
|
|
|
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....
|
|
|
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,...
|
|
|
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), R 1 independently at each occurrence is a C 1 –C 20 aliphatic radical, a C 3 –C 10 cycloaliphatic radical,...
|
|
|
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...
|
|
|
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...
|
|
|
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.
|
|
|
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...
|
|
|
7153946 |
Molecular conjugates for use in treatment of cancer
A molecular conjugate is provided having the formula:
wherein R 1 is a de-hydroxyl or de-amino moiety respectively of a hydroxyl-bearing or amino-bearing biologically active molecule or an...
|
|
|
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...
|
|
|
7151108 |
[3,4-a:3,4-c]carbazole compounds
A compound selected from those of formula (I):
wherein:
W 1 represents, together with carbon to which it is bonded, phenyl, pyridyl, Z represents a group of formula U—V as defined in...
|
|
|
7144876 |
3,5-Disubstituted-[1,2,4]-oxadiazoles and analogs as activators of caspases and inducers of apoptosis and the use thereof
Disclosed are 3,5-disubstituted-[1,2,4]-oxadiazoles and analogs thereof, represented by the Formula I:
wherein Ar 1 , R 2 , A, B and D are defined herein. The present invention relates to the...
|
|
|
7105492 |
Camptothecin derivatives having antitumor activity
Camptothecin derivatives of camptothecin of formula (I)
exhibit antitumor activity and show a good therapeutic index and are used in the treatment of tumors, viral infections and antiplasmodium...
|
|
|
7071203 |
Pharmaceutically acceptable salts of 20(s)-camptothecins
Described are pharmaceutically acceptable salts of a compound of formula (I)
its tautomeric forms, its stereoisomers or its polymorphs, which is obtained by treating the compound of formula (I)...
|
|
|
7060828 |
Liposomal camptothecins and uses thereof
This invention relates to improved liposomal camptothecin compositions and methods of manufacturing and using such compositions for treating neoplasia and for inhibiting angiogenesis.
|
|
|
7030243 |
Process for making camptothecin derivatives
A process for synthesizing highly lipophilic derivatives of camptothecin. The process includes reacting dissolved, underivatized camptothecin with a silylated heterocyclic compound in a modified...
|
|
|
7012079 |
Optically pure camptothecin analogues
The invention relates in particular to the compounds of general formula
in which R 1 , R 2 , R 3 , R 4 , R 5 , R 6 represent various radicals; their use as medicaments and pharmaceutical...
|
|
|
6992089 |
Nitro and amino substituted topoisomerase agents
The invention provides compounds of formula I:
wherein R 1 -R 9 , W, and X have any of the meanings defined in the specification and their pharmaceutically acceptable salts. The invention also...
|
|
|
6992088 |
Nitro and amino substituted heterocycles as topoisomerase I targeting agents
The invention provides compounds of formula I:
wherein: R 1 -R 5 , “a” and X have any of the meanings defined in the specification and their pharmaceutically acceptable salts. The...
|
|
|
6987109 |
Solubilized topoisomerase poison agents
The invention provides compounds of formula I:
wherein
A, B, W, Y, Z, and R 1 have any of the meanings defined in the specification and their pharmaceutically acceptable salts. The...
|
|
|
6967215 |
Tetrahydrocarbazoles, a process for the preparation of those compounds, and the use thereof
Tetrahydrocarbazoles of formula
where Q is —SO 2 —; —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,...
|
|
|
6964964 |
Topoisomerase poison agents
The invention provides compounds of formula I:
wherein
A, B, W, Y, Z, R 1 , R 3 and R 4 have any of the meanings defined in the specification and their pharmaceutically acceptable...
|
|
|
6933302 |
Nitrogen-based homo-camptothecin derivatives
(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,...
|
|
|
6916800 |
Combination therapy including a matrix metalloproteinase inhibitor and an antineoplastic agent
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.
|
|
|
6897200 |
Oligonucleotide delivery systems for camptothecins
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...
|
|
|
6893668 |
Process for isolation of anticancer agent camptothecin from Nothapodytes foetida
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)...
|
|
|
6872829 |
Process for the direct preparation of 5-alkoxy and 5-acyloxy analogues of camptothecins or mappicene ketones
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...
|
|
|
6858598 |
Method of using a matrix metalloproteinase inhibitor and one or more antineoplastic agents as a combination therapy in the treatment of neoplasia
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,...
|