|
Match
|
Document |
Document Title |
|
|
7560483 |
Methods for synthesis of prodrugs from 1-acyl-alkyl derivatives and compositions thereof
The present invention provides a method for synthesizing 1-(acyloxy)-alkyl derivatives from 1-acyl-alkyl derivatives, which typically proceeds stereospecifically, in high yield, does not require...
|
|
|
7534766 |
Glucuronide metabolites and epimers thereof of tigecycline
A glucuronide metabolite of tigecycline, and its corresponding epimer, have been identified in humans treated with tigecycline. Mass spectral data have been used to identify these structures.
|
|
|
7485707 |
Thermally stable crystalline epirubicin hydrochloride and method of making the same
A crystalline form of epirubicin hydrochloride, named herein as “type II” crystalline epirubicin hydrochloride, has excellent thermal stability. Type II crystalline epirubicin hydrochloride has...
|
|
|
7445764 |
Carrier-drug conjugate
The invention relates to a carrier-drug conjugate comprising a carrier containing a polypeptide sequence having one or several cysteine radicals and a pharmacon containing a pharmaceutical and/or...
|
|
|
7402556 |
Prodrugs activated by plasmin and their use in cancer chemotherapy
The product of the invention is a modified form of a therapeutic agent and comprises a therapeutic agent, an oligopeptide having a plasmin peptide substrate of 2-4 amino acids and mono- or...
|
|
|
7388083 |
Epimerization of 4′-C bond and modification of 14-CH3-(CO)-fragment in anthracyclin antibiotics
A method of synthesizing R1, R2-substituted-4′ (ax. or eq.)-OH anthracyclines and their corresponding salts of Formula (1) from daunorubicin or N-Trifluoroacetyl-4-R1-derivatives of daunorubicin,...
|
|
|
7345023 |
Treatment of hyperproliferative conditions of body surfaces
The present invention relates to pharmaceutical formulations comprising an anthracycline and the uses thereof for treatment of clinical conditions of body surfaces such as skin and mucosal...
|
|
|
7244829 |
Compositions and processes for preparing 13-deoxy-anthracyclines
13-benzenesulfonylhydrazone anthracyclines useful in producing improved yields in the synthesis 13-deoxyanthrcyclines, and an improved method of reducing 13-benzene-sulfonylhydrazone anthracyclines...
|
|
|
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...
|
|
|
7115576 |
Water-soluble antibiotic comprising an amino sugar, in the form of a polysaccharide conjugate
The invention relates to novel pharmaceutical forms for antibiotics containing amino sugar, amphotericin B, daunorubicin and doxorubicin, in which the known side effects are reduced and which can...
|
|
|
7109177 |
Methods and compositions for the manufacture of C-3′ and C-4′ anthracycline antibiotics
The present invention discloses new and novel substituted anthracyclines with modified alkyl-aromatic ring substitutions on the C-3′ of the sugar moiety or modified or unmodified alkyl-aromatic...
|
|
|
7091188 |
Stabilization of amrubicin hydrochloride
A stabilized amrubicin hydrochloride composition which comprises 3 to 8 wt. % water and 92 to 97 wt. % amrubicin hydrochloride; and a method of storing amrubicin hydrochloride.
|
|
|
7053191 |
Method of preparing 4-R-substituted 4-demethoxydaunorubicin
A method of synthesizing 4-R-substituted anthracyclines and their corresponding salts from 4-demethyldaunorubicin includes the steps of treating 4-demethyldaunorubicin with a sulfonylating agent to...
|
|
|
7005421 |
Injectable ready-to-use solutions containing an antitumor anthracycline glycoside
According to the invention there is provided a sterile, pyrogen-free, ready-to-use solution of an anthracycline glycoside, especially doxorubicin, which consists essentially of a physiologically...
|
|
|
6927211 |
Method for reducing toxicity of combined chemotherapies
Compositions and methods are provided for use in the treatment of cancer.
|
|
|
6921841 |
Process for the synthesis of optically active anthracyclines
It is described a process for the synthesis of optically active anthracyclines by the fact that the key intermediate (R)2-acetyl-2-hydroxy-1,2,3,4-tetrahydronaphtalene...
|
|
|
6914046 |
NF-κB activation inhibitors, and their pharmaceutical uses
Compounds inhibiting the activation of the nuclear factor κB (NF-κB) are used for the preparation of medications adapted for the treatment of malignant hemopathies and solid tumors, and for the...
|
|
|
6844318 |
Peptidase-cleavable, targeted antineoplastic drugs and their therapeutic use
This invention is directed to antineoplastic agents conjugated to enzyme-cleavable peptides comprising the amino acid recognition sequence of a membrane-bound and/or cell-secreted peptidase, and to...
|
|
|
6720306 |
Tetrapartate prodrugs
A compound of Formula I, providing tetrapartate prodrugs is provided wherein: L 1 is a bifunctional linking moiety; D is a moiety that is a leaving group, or a residue of a compound to be...
|
|
|
6716821 |
Cytotoxic agents bearing a reactive polyethylene glycol moiety, cytotoxic conjugates comprising polyethylene glycol linking groups, and methods of making and using the same
Cytotoxic agents bearing a polyethylene glycol (PEG) linking group having a terminal active ester, cytotoxic conjugates comprising one or more cytotoxic agents linked to a cell-binding agent via...
|
|
|
6709679 |
Antineoplastic conjugates of transferin, albumin and polyethylene glycol
Conjugates of transferrin, albumin and polyethylence glycol consisting of native or thiolated transferrin or albumin or of polyethylene glycol (MW between approximately 5,000 and 20,0000) with at...
|
|
|
6680300 |
Methods and compositions for the manufacture of highly potent anthracycline-based antitumor agents
The present invention discloses new and novel substituted anthracyclines having a three ring system or other DNA binding moieties. These congeners show high activity in vitro against several tumor...
|
|
|
6677309 |
Anti-cancer drug aldehyde conjugate drugs with enhanced cytotoxicity compounds, compositions and methods
Monomeric and dimeric anti-cancer drug aldehyde conjugate compounds and pharmaceutically acceptable salts thereof. Specifically, monomeric and dimeric aldehyde conjugates of 1-2,...
|
|
|
6673907 |
Methods and compositions for the manufacture of C-3′ and C-4′ anthracycline antibiotics
The present invention discloses new and novel substituted anthracyclines with modified alkyl-aromatic ring substitutions on the C-3′ of the sugar moiety or modified or unmodified alkyl-aromatic...
|
|
|
6670348 |
Methods and compositions for destruction of selected proteins
Compounds having an ansamycin anitibiotic, or other moiety which binds to hsp90, coupled to a targeting moiety which binds specifically to a protein, receptor or marker can provide effective...
|
|
|
6653455 |
Crystallization of doxorubicin hydrochloride
Disclosed are a crystallizing method of doxorubicin hydrochloride from a doxorubicin hydrochloride-containing solution, particularly a method for carrying out the crystallization under a condition...
|
|
|
6653289 |
L-arabino-disaccharides of anthracyclines, processes for their preparation, and pharmaceutical compositions containing them
The present invention refers to compounds of general formula (I), the pharmaceutically acceptable salts thereof, the processes for their preparation, and the pharmaceutical compositions containing...
|
|
|
6630579 |
Cytotoxic agents comprising modified doxorubicins and daunorubicins and their therapeutic use
A cytotoxic agent comprising one or more modified doxorubicins/daunorubicin linked to a cell binding agent. A therapeutic composition for killing selected cell populations comprising: (A) a...
|
|
|
6624142 |
Trimethyl lock based tetrapartate prodrugs
The invention is directed primarily to compounds of Formula I: wherein: R 1 is a polymeric residue; L 1 is a bifunctional linking group; Y 1 and Y 2 are independently O, S or NR 7 ; R 2-7 ...
|
|
|
6500936 |
Pluraflavins and derivatives thereof, process for their preparation and use thereof
The invention relates to a compound of formula (I) wherein R 1 is a sugar; R 2 is —CH 2 —O—(R 7 )m, R 7 representing a sugar, or is —COOH; R 3 is an epoxide-comprising group, or is C...
|
|
|
6433150 |
Anthracycline analogues bearing latent alkylating substituents
Compound having the structure where anthracycline, N, R a , X, R b, n and m are as defined in the specification. The compound of the invention is activatable in vivo by esterases and...
|
|
|
6399583 |
Hybrid anthracyclines from genetically engineered streptomyces galilaeus strains, process for production and uses thereof
The present invention relates to novel hybrid anthracyclines generated by cloning of fused genes in a mutated Streptomyces galilaeus strain DSM 11638. Said strain was obtained by mutagenization...
|
|
|
6391305 |
Conjugates useful in the treatment of prostate cancer
Chemical conjugates which comprise oligopeptides, having amino acid sequences that are selectively proteolytically cleaved by free prostate specific antigen (PSA), hydrophilic oligopeptide blocking...
|
|
|
6388058 |
Method of purifying daunomycin
The present invention relates to a method in which daunomycin is eluted from a hydrophobic porous synthetic resin carrier onto which daunomycin is adsorbed from crude daunomycin with a buffered...
|
|
|
6376469 |
Crystalline amrubicin hydrochloride
β-Type crystalline amrubicin hydrochloride having a powder X-ray diffraction pattern having average values of diffraction angle(2θ) and relative intensity as given in the following table: ...
|
|
|
6355784 |
Methods and compositions for the manufacture of halogenated anthracyclines with increased antitumor activity, other anthracyclines, halogenated sugars, and glycosyl donors
The present invention discloses new and novel halogenated anthracyclines linked through the saccharide portions. These congeners show high activity in vitro against several tumor cell lines. In...
|
|
|
6303569 |
Trialkyl-lock-facilitated polymeric prodrugs of amino-containing bioactive agents
The present invention is directed to double prodrugs containing polymeric-based transport forms. These polymeric compounds comprise the formula: ##STR1## wherein: B is H, OH, OSiR 13 , a...
|
|
|
6284737 |
Methods of treatment with anthracycline derivatives
The present invention is a compound having the structure ##STR1## where: anthracycline is doxorubicin, daunorubicin or a derivative thereof; N is the 3' nitrogen of daunosamine; R a is H...
|
|
|
6281342 |
Pradimicin compounds
Disclosed are novel pradimicin compounds which possess antifungal activity and, preferably, improved water solubility. The compounds of the invention are prepared by modifying the 4'-amino or...
|
|
|
6258786 |
13-dihydro-3' aziridino anthracyclines
The present invention relates to anthracycline glycosides, to a process for their preparation and to pharmaceutical compositions containing the same.
|
|
|
6218519 |
Compounds and methods for the selective treatment of cancer and bacterial infections
The present invention relates to compounds containing an anthracyclinone group such as doxorubicin, daunorubicin or a derivative thereof. The compounds of the invention also contain ester,...
|
|
|
6187758 |
Anthracycline glycosides
An anthracycline glycoside of formula I ##STR1## wherein R is one of the two following residues: ##STR2## or a pharmaceutically acceptable salt thereof.
|
|
|
6184365 |
Anthracycline derivatives having 4-amino-2,4,6-trideoxy-2 fluoro-α-L-talopyranosyl group
7-O-(4-Amino-2,4,6-trideoxy-2-fluoro-α-L-talopyranosyl)-dau
nomycinone or -adriamycinone is now synthesized as a novel daunomycinone or adriamycinone derivative having the general formula ##STR1##...
|
|
|
6180095 |
Polymeric prodrugs of amino- and hydroxyl-containing bioactive agents
The present invention is directed to double prodrugs containing polymeric-based transport forms. These polymeric prodrugs are preferably of the formula: ##STR1## wherein: L 1 is a bifunctional...
|
|
|
6177404 |
Conjugates useful in the treatment of benign prostatic hyperplasia
Novel pharmaceutical compositions useful for the treatment of benign prostatic hyperplasia which comprises novel oligopeptides, which are selectively cleaved by enzymatically active PSA, in...
|
|
|
6160102 |
Oligonucleotide-anthracycline and oligonucleotide-anthracyclinone conjugates
The present invention refers to conjugates formed by a natural or modified oligonucleotide, capable of forming a triple helix with a DNA chain, linked to the aglycone moiety of an anthracycline or...
|
|
|
6103700 |
Fluoro labelled anthracyclinone and anthracycline derivatives
Compounds of formula (A), wherein R 1 , R 2 , R 3 , Y and Z are organic substituents, are useful in the diagnosis of amyloidosis; some of the compounds of formula (A) are novel. Processes for their...
|
|
|
6080396 |
Anthracycline compound derivative and pharmaceutical preparation containing the same
A dimer, trimer or tetramer of an anthracycline compound which can be obtained by directly, chemically bonding anthracycline compounds having anticancer activities to each other by an alkali...
|
|
|
6075135 |
3,4-di-O,N-Protected-4-amino-2,4,6-trideoxy-2-fluoro-L-manno-pyranosyl halide and a process for its preparation
7-O-(4-Amino-2,4,6-trideoxy-2-fluoro-α-L-mannopyranosyl)-da
unomycinon e or -adriamycinone is now synthesized as a daunomycinone or adriamycinone derivative having the general formula ##STR1##...
|
|
|
6020316 |
Glutaraldehyde modified chemotherapeutic agents and methods of use thereof
Clinical utility of chemotherapy agents is limited by dose-dependent systemic toxicity and emergence of resistant tumor cell lines. The present invention provides derivatives of chemotherapeutic...
|