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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...
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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...
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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...
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7598279 |
Neurotherapeutic azole compounds
Azole compounds containing carbamoyl group and pharmaceutically useful salts thereof are described. The compounds are effective anticonvulsants which are used in the treatment of disorders of the...
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7595347 |
Method for protecting normal cells from cytotoxicity of chemotherapeutic agents
Pre-treatment with α,β unsaturated aryl sulfones protects normal cells from the cytotoxic side effects of two classes of anticancer chemotherapeutics. Administration of a cytoprotective sulfone...
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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...
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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,...
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7557118 |
Preparation of fused polycyclic alkaloids by ring closure of azomethine ylides, novel compounds thereof and their use as chemotherapeutic agents
A method for the preparation of a compound of general Formula:
or pharmaceutically acceptable derivatives and salts, racemates, isomers and/or tautomers thereof comprising cyclizing an...
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7517891 |
Camptothecin derivatives and improved synthetic methods
The present invention relates to compositions and methods for preparing pharmaceutical compositions. In some embodiments, the invention includes compounds and methods of resolving chiral compounds....
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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...
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7498334 |
Pyrrolopyrimidines as phosphodiesterase VII inhibitors
Pyrrolopyrimidine derivatives of the formula I
in which R 3 , R 4 , R 5 , R 6 and X are as defined in claim 1 , act as phosphodiesterase VII inhibitors and can be employed for the treatment...
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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...
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7485320 |
Liposome for incorporating large amounts of hydrophobic substances
A liposome formulation for stably incorporating high content of hydrophobic substance is disclosed. The liposome includes two phospholipids with different phase transition temperatures such as...
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7482359 |
Androgen receptor modulators
Compounds of structural Formula (I) are modulators of the androgen receptor (AR) in a tissue selective manner These compounds are useful in the enhancement of weakened muscle tone and the treatment...
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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.
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7455853 |
Medical devices containing rapamycin analogs
A medical device comprising a supporting structure capable of containing or supporting a pharmaceutically acceptable carrier or excipient, which carrier or excipient may contain one or more...
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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...
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7396837 |
Antitumoral analogs of lamellarins
New lamellarins are provided of the general formula III or a pharmaceutically acceptable salt, derivative, prodrug or stereoisomer thereof
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7354918 |
Derivatives of 14.15-dihydro 20.21-dinoreburnamenin-14-ol and applications thereof
The invention relates to novel derivatives of 14,15-dihydro 20,21-dinoreburnamenin-14-ol, having formula (I)
in which R represents a radical —AR′ wherein A represents a heteroatom and R′...
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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...
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7348025 |
Small particle liposome aerosols for delivery of anticancer drugs
Provided herein is a method of treating primary lung cancer or metastatic cancer to the lung in an individual by delivering at least once to the respiratory tract of the individual via inhalation a...
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7345046 |
Heteroaryl-fused pyrimidinyl compounds as anticancer agents
Heteroaryl-fused pyrimidinyl compounds, pharmaceutically acceptable salts, and prodrugs thereof; compositions that include a pharmaceutically acceptable carrier and one or more of the...
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7332502 |
Phenanthroindolizidine alkaloids
A group of novel phenanthroindolizidine alkaloid compounds as shown and their use in treating cancer. Also disclosed are methods of using phenanthroindolizidine alkoid compounds in suppressing NO...
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7304037 |
Cytostatic conjugates with integrin ligands
The present invention relates to cytostatics which have a tumor-specific action as a result of linkage to α v β 3 integrin antagonists via preferred linking units which can be selectively...
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7285533 |
Apo-2 ligand
A novel cytokine, designated Apo-2 ligand, which induces mammalian cell apoptosis is provided. The Apo-2 ligand is believed to be a member of the TNF cytokine family. Compositions including Apo-2...
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7276252 |
Method and form of a drug delivery device, such as encapsulating a toxic core within a non-toxic region in an oral dosage form
A drug delivery device such as an oral dosage form (ODF) with a toxic or potent core encapsulated by a non-toxic region. The non-toxic region may be a region including multiple layers, coatings,...
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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,...
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7250422 |
Pharmaceutical composition containing berberine as effective ingredient for preventing and treating addiction or tolerance to morphine
Disclosed is a pharmaceutical composition for preventing and treating addiction to morphine or preventing and inhibiting the development of tolerance to the analgesic effects of morphine,...
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7238704 |
Vinca derivatives
The present invention relates to derivatives of vinca alkaloids. Pharmaceutical compositions containing these compounds as well as processes of preparation and treatment of various conditions are...
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7235564 |
Vinorelbine derivatives
The present invention relates to novel vinorelbine derivatives. Pharmaceutical compositions containing these compounds as well as processes of preparation and processes of use for treatment of...
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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...
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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...
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7217770 |
Stable polymeric micelle-type drug composition and method for the preparation thereof
A biocompatible stable composition containing a hydrophobic drug, such as paclitaxel. The composition, which forms a syringeable polymeric micellar solution in aqueous or body fluids, is a...
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7163930 |
Pharmaceutical compositions and methods relating to fucans
Compositions, methods and the like comprising fucans such as fucoidan to treat surgical adhesions, arthritis, and psoriasis.
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7163703 |
Compositions and methods for the treatment of primary and metastatic neoplastic diseases using arsenic compounds
The invention relates to the use of arsenic compounds to treat a variety of neoplastic diseases. The present invention encompasses the administration to a mammal of arsenic in the form of a salt,...
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7122553 |
Liposomal formulation of irinotecan
The present invention is for novel compositions and methods for treating cancer, particularly, for treating cancer in mammals and more particularly in humans. The therapeutic compositions of the...
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7119124 |
Pharmaceutical compositions containing plasma protein
The invention is related to water-soluble products and pharmaceutical formulations in solid or liquid form mainly for parenteral use. They consist of or comprise a therapeutically active substance...
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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...
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7091189 |
Medicament for treating lung cancer
By using a combination of amrubicin or a pharmaceutically acceptable salt thereof with another medicament for treating lung cancer (irinotecan, vinorelbine, gemcitabine, etc.), it is intended to...
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7078411 |
Phospholipid transfer protein (PLTP) and cholestoral metabolism
A method for controlling cholesterol metabolism in a host, a screening assay for agents that can control cholesterol metabolism, and the agents that may be identified are practiced and determined...
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7078209 |
CAK inhibitors and uses thereof
The present invention relates to compounds useful as inhibitors of CAK, compositions thereof. The present invention also relates to methods using the compositions for treating CAK-mediated...
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7071204 |
Camptothecin analogs having an E-ring ketone
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...
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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)...
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7071202 |
Compositions and formulations of 9-nitrocamptothecin polymorphs and methods of use therefor
A polymorphic form of 9-nitrocamptothecin is provided, the polymorph being characterizable as having, by differential scanning calorimetry, no observable endotherm and an exotherm at between 273.6...
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7053102 |
Analogues of camptothecin, their use as medicaments and the pharmaceutical compositions containing them
Compositions for treating cancer comprising an amount of a camptothecin with a 7-ring β-hydroxy lactone ring of the formula
wherein the substituents are defined as in the specification...
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7049322 |
Compositions and formulations of 9-nitrocamptothecin polymorphs and methods of use therefor
A polymorphic form of 9-nitrocamptothecin is provided, the polymorph being characterizable as having, by differential scanning calorimetry, an endotherm at between 273.9 to 275.9° C., and an...
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7044624 |
Vehicle light with movable reflector portion and shutter portion for selectively switching an illuminated area of light incident on a predetermined portion of the vehicle light during driving
A vehicle light can include a light source, a major reflecting surface, a projection lens, and a shutter. A first reflecting surface of an ellipse group reflecting surface preferably has a first...
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7034024 |
Product inhibiting transduction of G heterotrimeric protein signals combined with another anti-cancer agent for therapeutic use in cancer treatment
The invention concerns a product inhibiting transduction of G heterotrimeric protein signals combined with another anti-cancer agent, in particular farnesyltransferase inhibitors, taxol or...
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7026301 |
Method of orally treating inflammatory skin conditions with prodrugs of 5-fluorouracil
The present invention relates to the treatment of inflammatory skin conditions, including psoriasis, with a prodrug of 5-fluorouracil. The invention relates to methods for treatment of psoriasis...
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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...
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