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Class 514/283 - Ring nitrogen in the pentacyclo ring system is shared by five-membered cyclo and six-membered cyclo (e.g., vincamine, etc.)


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter wherein the ring nitrogen of the six-membered
No. of patents: 387
Last issue date: 05/01/2012


1                    
NumberTitleIssue Date
8168648Camptothecin derivatives and uses thereof
The present invention provides two new camptothecin derivatives, which were identified as S,R- and S,S-topotecan lactates, respectively. Both compounds have anticancer activities. Pharmaceutical compositions of the new camptothecin derivatives, and cancer therapies ...
05/01/2012
8158645Compound, corresponding compositions, preparation and/or treatment methods
Disclosed is a novel crystalline form of topotecan monohydrochloride pentahydrate, which is a pentahydrate of 10-[(dimethylamino)methyl]-4-ethyl-4,9-dihydroxy-1H-pyrano[3′,4′:6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)dione monohydrochloride, corresponding pharm...
04/17/2012
8138200Compositions and methods for double-targeting virus infections and targeting cancer cells
The invention includes compositions and methods useful for treatment of a virus infection in a mammal by double-targeting the virus (i.e. targeting the virus at more than one stage of the virus life cycle) and thereby inhibiting virus replication. The compositions o...
03/20/2012
80805595(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 5(RS)-(2′-hydroxyethoxy)-20(S)-camptothecin, or the 5(R)-(2′-hydroxyethoxy)-20(S)-camptothecin dias...
12/20/2011
8048891Treatment of non-hodgkin's lymphomas with multi-arm polymeric conjugates of 7-ethyl-10-hydroxycamptothecin
The present invention relates to methods of treatment of non-Hodgkin's lymphomas. The present invention includes administering polymeric prodrugs of 7-ethyl-10-hydroxycamptothecin to patients in need thereof. ...
11/01/2011
8026250Compositions for delivering highly water soluble drugs
The present invention provides compositions for delivering highly water-soluble drugs (such as vinca alkaloids) and methods of using such compositions. ...
09/27/2011
8026249Deuterium-enriched topotecan
The present application describes deuterium-enriched topotecan, pharmaceutically acceptable salt forms thereof, and methods of treating using the same. ...
09/27/2011
7994186Pharmaceutical compositions containing camptothecins
A camptothecin-containing pharmaceutical composition which contains: (a) camptothecin or a derivative thereof, and (b) one or more compounds selected from among ascorbic acid or a salt thereof, sodium hydrogen sulfite, sodium sulfite, potassium pyrosulfite, sodium e...
08/09/2011
7989421Use of dimiracetam in the treatment of chronic pain
The use of dimiracetam in the treatment of chronic pain is disclosed. At doses higher than those previously disclosed in relation with its cognition enhancing activity (i.e. amelioration of learning and memory), dimiracetam was able to completely revert hyperalgesia...
08/02/2011
7888368Treatment of drug-resistant tumors
A subclass of camptothecin derivatives is disclosed to be useful for the preparation of a medicament for the treatment of drug-resistant tumors and/or for the administration to patients who show polymorphisms in the gene coding for DNA topoisomerase I. ...
02/15/2011
7786134Lipophilic anticancer drug compounds, compositions and related methods
Lipophilic anticancer drug compounds, compositions that include the compounds, and methods for treating a cell proliferative disease using the compounds. ...
08/31/2010
7754733Crystalline topotecan hydrochloride product and process for making the same
Disclosed is a novel crystalline form of topotecan monohydrochloride pentahydrate, which is a pentahydrate of 10-[(dimethylamino)methyl]4-ethyl-4,9-dihydroxy-1H-pyrano[3′,4′:6,7]indolizino[1,2-b]quinoline-3,14(4H, 12H)dione monohydrochloride, corresponding pharm...
07/13/2010
7723351Multi-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. ...
05/25/2010
7705012Camptothecins conjugated in position 7 to cyclic peptides as cytostatic agents
Compounds of Formula (I) are described in which the R1 group is as defined in the specification and includes the condensation of the camptothecin molecule in position 7 with a cyclopeptide containing the RGD sequ...
04/27/2010
7700612Di-ester prodrugs of camptothecin, process for their preparation and their therapeutical applications
The present invention is related to 10,20-di-O ester derivatives of camptothecin and pharmaceutical formulations thereof. The compounds and pharmaceutical formulations of the present invention possess increased biological life span and bioavailability and reduced to...
04/20/2010
7700613Use of 7-t-butoxyiminomethylcamptothecin for the preparation of a medicament for the treatment of uterine neoplasms
The use of 7-ter-butoxyiminomethylcamptothecin is described in the preparation of a medicament useful for the treatment of uterine neoplasms, particularly cancer of the endometrium and of the neck of the womb. ...
04/20/2010
7671067Treatment of non-hodgkin's lymphomas with multi-arm polymeric conjugates of 7-ethyl-10-hydroxycamtothecin
The present invention relates to methods of treatment of non-Hodgkin's lymphomas. The present invention includes administering polymeric prodrugs of 7-ethyl-10-hydroxy-camptothecin to patients in need thereof. ...
03/02/2010
7652027Phenanthroindolizidine 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 and TNF-α production, inhibiting MEKK1 activity and cyclooxygenase II...
01/26/2010
7638528Compositions and methods for targeting cancer cells
The invention includes compositions and methods useful for treatment of a virus infection in a mammal by double-targeting the virus (i.e. targeting the virus at more than one stage of the virus life cycle) and thereby inhibiting virus replication. The compositions o...
12/29/2009
76120817-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 residue, such amine groups bei...
11/03/2009
76017335(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 5(RS)-(2′-hydroxyethoxy)-20(S)-camptothecin, or the 5(R)-(2′-hydroxyethoxy)-20(S)-camptothecin dias...
10/13/2009
7601732Crystalline 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 diffraction pattern comprising one or more peak intensities expressed in ...
10/13/2009
75890997-t-butoxyiminomethylcamptothecin conjugated in position 20 with integrin antagonists
Compounds of Formula (I) are described: in which the R1 group is as defined in the specification and includes the condensation of 7-t-butoxyiminomethylcamptothecin in position 20 with a cyclopeptide containing th...
09/15/2009
7572803Hydrated 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, methods of treating a cancer or malignant tumor using the crystalline...
08/11/2009
7557118Preparation 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 azomethine ylide of general Formula:
07/07/2009
7517891Camptothecin 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. In some embodiments, the invention includes chiral and crystalline c...
04/14/2009
7498340Esters 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 mixtures, and their pharmaceutically acceptable salts. Said compounds...
03/03/2009
7482359Androgen 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 of conditions caused by androgen deficiency or which can be ameliora...
01/27/2009
7462627Multi-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. ...
12/09/2008
7452900Esters 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 mixtures, and their pharmaceutically acceptable salts. Said compounds...
11/18/2008
7399860Manufacture 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
7396837Antitumoral analogs of lamellarins
New lamellarins are provided of the general formula III or a pharmaceutically acceptable salt, derivative, prodrug or stereoisomer thereof ...
07/08/2008
7368440Methods for the administration of amifostine and related compounds
The present invention provides methods of administering amifostine, WR-1065, or a combination thereof, to patients receiving radiation therapy or chemotherapy in a manner that significantly reduces or decreases the adverse or undesirable side-effects of the compound...
05/06/2008
7354918Derivatives 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′ represents a group selected fr...
04/08/2008
73517147-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
7348025Small 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 nebulized liposomal aerosol comprising a dilauroylphosphatidylcholin...
03/25/2008
7348310Synthetic methods for aplidine and new antitumoral derivatives, methods of making and using them
The invention relates to aplidine derivatives of the general formula: which are useful for the treatment of tumors. ...
03/25/2008
7345046Heteroaryl-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 heteroaryl-fused pyrimidinyl compounds, either alone or in combination with at lea...
03/18/2008
7332502Phenanthroindolizidine 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 and TNF-α production, inhibiting MEKK1 activity and cyclooxygenase II...
02/19/2008
7304037Cytostatic conjugates with integrin ligands
The present invention relates to cytostatics which have a tumor-specific action as a result of linkage to αvβ3 integrin antagonists via preferred linking units which can be selectively cleaved by elastase, i.e. by an enzyme which can especial...
12/04/2007
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