Entries |
Document | Title | Date |
20080207728 | BICYCLIC ACYLTRYPTOPHANOLS - The present invention relates to acyltryptophanols of the general formula I, | 08-28-2008 |
20080221192 | Compounds and Compositions as Protein Kinase Inhibitors - The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, Bcr-Abl, cSrc, TPR-Met, Tie2, MET, FGFR3, Aurora, Axl, Bmx, BTK, c-kit, CHK2, Flt3, MST2, p70S6K, PDGFR, PKB, PKC, Raf, ROCK-H, Rsk1, SGK, TrkA, TrkB and TrkC kinases. | 09-11-2008 |
20080221193 | 3-AMINO CHROMANE DERIVATIVES - The present invention relates to 3-amino chromane derivatives; to compositions containing such compounds; to methods of synthesizing such compounds; and to methods of using such compounds and compositions containing such compounds in the treatment of serotonin disorders, such as depression and anxiety. | 09-11-2008 |
20080227841 | INTRAVESICAL APAZIQUONE ADMINISTRATION FOLLOWING TRANSURETHRAL RESECTION - Bladder cancer treatments include the intravesical administration of apaziquone immediately (e.g. within about 6 hours) following transurethral resection. | 09-18-2008 |
20080227842 | Non-fluorescent chlorophyll catabolites - The invention relates to a compound of formula (I), or a pharmacologically or cosmetically acceptable salt or derivative thereof, wherein R | 09-18-2008 |
20080227843 | THERAPEUTIC USE OF N-(1H-INDOLYL)-1H-INDOLE-2-CARBOXAMIDE DERIVATIVES - The invention relates to therapeutic use of compounds of general formula (I): | 09-18-2008 |
20080234355 | DNA METHYL TRANSFERASE INHIBITORS CONTAINING A ZINC BINDING MOIETY - The present invention relates to inhibitors of DNMT containing zinc moiety derivatives that have enhanced or unique properties as inhibitors of DNA methyl transferases (DNMT) and their use in the treatment of DNMT related diseases and disorders such as cancer. The said derivatives may further act as HDAC inhibitors. | 09-25-2008 |
20080275101 | Solid Salt Forms Of A Pyrrole Substituted 2-Indolinone - The present invention relates to solid salt forms of the 3-pyrrole substituted 2-indolinone compound 5-[5-fluoro-2-oxo-1,2-dihydro-indol-(3Z)-ylidenemethyl]-2,4-dimethyl-1H-pyrrole-3-carboxylic acid (2-pyrrolidin-1-yl-ethyl)-amide. It also relates to polymorphs of the phosphate salt of the amide. The invention further relates to the use of the salts and polymorphs in the treatment of protein kinase related disorders. | 11-06-2008 |
20080287519 | Amorphous eletriptan hydrobromide and process for preparing it and other forms of eletriptan hydrobromide - The invention encompasses amorphous eletriptan hydrobromide, processes for preparing it and pharmaceutical compositions of it. The invention also relates to processes for preparing other forms of eletriptan hydrobromide such as Form α and Form β. | 11-20-2008 |
20090012145 | THERAPEUTIC ESTERS - A compound comprising | 01-08-2009 |
20090048327 | Polymorphs of Pyrrole Substituted 2-Indolinone Protein Kinase Inhibitors - The present invention relates to polymorphs of the 3-pyrrole substituted 2-indolinone compound 5-(5-fluoro-2-oxo-1,2-dihydro-indol-3-ylidenemethyl)-2,4-dimethyl-1H-pyrrole-3-carboxylic acid (2-pyrrolidin-1-yl-ethyl)-amide. | 02-19-2009 |
20090062367 | DEUTERIUM-ENRICHED ELETRIPTAN - The present application describes deuterium-enriched eletriptan, pharmaceutically acceptable salt forms thereof, and methods of treating using the same. | 03-05-2009 |
20090062368 | DEUTERIUM-ENRICHED SUNITINIB - The present application describes deuterium-enriched sunitinib, pharmaceutically acceptable salt forms thereof, and methods of treating using the same. | 03-05-2009 |
20090076120 | Crystal of Aminopyrrolidine Derivative and Production Method Thereof - Two crystal forms of (R)-3-[2-(2-amino-5-trifluoromethoxybenzamido)acetamido]-1-(6-methylindol-3-ylmethyl)pyrrolidine which exhibit specific X-ray powder diffraction patterns or infrared absorption spectra, amorphous form thereof, a pharmaceutical composition containing the crystal or amorphous form as an active ingredient, as well as methods for preparing them are provided. | 03-19-2009 |
20090111867 | INDOLE ACETIC ACIDS EXHIBITING CRTH2 RECEPTOR ANTAGONISM AND USES THEREOF - The invention relates to indole acetic acid compounds which function as antagonists of the CRTH2 receptor. The invention also relates to the use of these compounds to inhibit the binding of prostaglandin D | 04-30-2009 |
20090131502 | Biologically active compounds - The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of a disease selected from osteoporosis, Paget's disease, Chagas's disease, malaria, gingival diseases, hypercalaemia, metabolic bone disease and diseases involving matrix or cartilate degradation. | 05-21-2009 |
20090131503 | 3,5 - SUBSTITUTED INDOLE COMPOUNDS HAVING NOS AND NOREPINEPHRINE REUPTAKE INHIBITORY ACTIVITY - The present invention relates to novel 3,5-substituted indole compounds of Formula (I) having nitric oxide synthase (NOS) inhibitory activity together with inhibitory activity at the norepinephrine transporter (NET), to pharmaceutical and diagnostic compositions containing them, and to their medical use. | 05-21-2009 |
20090163570 | BLADDER CANCER TREATMENT AND METHODS - Disclosed herein are various bladder cancer treatments and methods. The present disclosure can take advantage of propylene glycol concentrations and/or NAD(P)H:quinone oxidoreductase-1 (NQO1), Cytochrome P450 Oxidoreductase (P450R) and Glucose transporter 1 (Glut-1) protein expression in human transitional cell carcinoma of the bladder to offer individually targeted bladder cancer treatments. | 06-25-2009 |
20090176856 | MUSCARINIC RECEPTOR ANTAGONISTS - This present invention generally relates to muscarinic receptor antagonists, which are useful, among other uses, for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. The invention also relates to the process for the preparation of disclosed compounds, pharmaceutical compositions containing the disclosed compounds, and the methods for treating diseases mediated through muscarinic receptors. | 07-09-2009 |
20090186933 | INDOLE, AZAINDOLE AND RELATED HETEROCYCLIC PYRROLIDINE DERIVATIVES - This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with amido piperazine derivatives. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS. | 07-23-2009 |
20090258920 | INJECTABLE FORMULATION OF ANTIBIOTIC AND SOLUTION FOR INTRAVENOUS ADMINISTRATION THEREOF - A pharmaceutical composition for injection comprising a depsipeptide antibiotic, WAP-8294A | 10-15-2009 |
20090258921 | INDOLE DERIVATIVES - Novel indole derivatives of formula (I) or a pharmaceutically acceptable salt thereof: | 10-15-2009 |
20090264494 | USE OF NEUROPROTECTIVE 3-SUBSTITUTED INDOLONE COMPOSITIONS - The present invention include providing a therapeutically effective amount of a 3-substituted indolin-2-one compositions to protect against neurodegeneration including diseases such as Alzheimer's disease, Parkinson's disease, or Huntington's disease, and conditions such as ischemic stroke | 10-22-2009 |
20090286846 | Therapeutic use of N-(1H-Indolyl)-1H-indole-2-carboxamide derivatives - The invention relates to therapeutic use of compounds of general formula (I): | 11-19-2009 |
20090291998 | EPONEMYCIN AND EPOXOMICIN ANALOGS AND USES THEREOF - The present invention provides compounds having formula (1): wherein R | 11-26-2009 |
20090298904 | NOVEL PEPTIDES FROM ACTINOMADURA NAMIBIENSIS - The disclosure relates to a compound of the formula (I) | 12-03-2009 |
20090312390 | INHIBITORS OF GLYCOGEN SYNTHASE KINASE-3 (GSK-3) FOR TREATING GLAUCOMA - The use of inhibitors of GSK-3 useful for treating glaucoma is disclosed. | 12-17-2009 |
20090318525 | Process For Preparing A 3-Pyrrole Substituted 2-Indolinone Malate Salt - The invention relates to the malic acid salt of N-[2-(diethylamino)ethyl]-5-formyl-2,4-dimethyl-1H-pyrrole-3-carboxamide, to the use thereof as an intermediate for preparing the malic acid salt of sunitinib, and to pharmaceutical compositions comprising said malic acid salt of sunitinib. | 12-24-2009 |
20100004308 | Benzofuran-3-yl(indol-3-yl) Maleimides as Potent GSK3 Inhibitors - Compounds of formula: | 01-07-2010 |
20100048662 | Novel Pyrone-Indole Derivatives and Process for Their Preparation - The present invention relates to novel pyrone-indole derivatives, pharmaceutical formulations containing them, and use of the compounds in the manufacture of Medicaments for treating or preventing various diseases. | 02-25-2010 |
20100076049 | NOVEL OXINDOLE DERIVATIVE - A compound or a pharmaceutically acceptable salt thereof of the present invention is represented by the following general formula (I): | 03-25-2010 |
20100099731 | Use of Endothelial Interrupters in the Treatment of Neurodegenerative Diseases - In various embodiments, the present invention relates generally to methods of treating at least one neurodegenerative disease by administering a medicament comprising an endothelial interrupter. | 04-22-2010 |
20100113555 | Modulators of ATP-Binding Cassette Transporters - Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention. | 05-06-2010 |
20100120885 | Novel Derivatives of Psammaplin A, A Method For Their Synthesis And Their Uses For The Prevention Or Treatment Of Cancer - Derivatives of psammaplin A responding to formula (I), a method for their synthesis and their use for the preparation of a medicament for preventing and for treating a tumor or a cancer. Formula (I). | 05-13-2010 |
20100130581 | COMPOUNDS AND METHODS FOR THE TREATMENT OF PAIN - This invention relates to derivatives of an endomorphin, or of an endomorphin analog, comprising at least one moiety selected from a lipid moiety, a cyclitol moiety and a saccharide moiety. | 05-27-2010 |
20100144821 | COMPOUNDS AND METHODS FOR TREATING PROTEIN FOLDING DISORDERS - The invention is directed to compounds and methods for treating protein folder disorders. In certain embodiments the invention provides compounds and methods for treating neurodegenerative diseases such as Alzheimer's disease, tauopathy, cerebral amyloid angiopathy, Lewy body disease, dementia, Huntington's disease and prion-based spongiform encelopathy. The invention further provides compounds, methods and pharmaceutical compositions for inhibiting tau protein, Aβ protein or α-synuclein protein aggregation. | 06-10-2010 |
20100144822 | Use of Inhibitors of the Degradation of P27, in Particular Argyrin and Derivatives Thereof, for the Treatment of Proliferative Diseases - The present invention relates to the use of particular macrocycles that are inhibitors of the proteasomic degradation of p27, in particular Argyrin and derivatives thereof, preferably Argyrin A, for the treatment of proliferative diseases, such as cancer, as well as the derivatization of said macrocycles. | 06-10-2010 |
20100144823 | NOVEL INDOLE DERIVATIVES AS SELECTIVE ANDROGEN RECEPTOR MODULATORS (SARMS) - The present invention is directed to novel indole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor. | 06-10-2010 |
20100152270 | PESTICIDE COMPOSITION COMPRISING A STRIGOLACTONE DERIVATIVE AND A FUNGICIDE COMPOUND - A composition comprising at least a strigolactone derivative (a) of general formula: | 06-17-2010 |
20100179207 | COMPOUNDS - The present invention pertains generally to certain compounds of the deoxyactagardine A and B type. Such compounds are suitable for use in the treatment of microbial infections, for example | 07-15-2010 |
20100273852 | PHARMACEUTICAL COMPOSITION - There is provided a pharmaceutical composition comprising (1) (R)-5,6-dimethoxy-2-[2,2,4,6,7-pentamethyl-3-(4-methylphenyl)-2,3-dihydro-1-benzofuran-5-yl]isoindoline, (2) a lipophilic component, and (3) a surfactant, which can stably and sufficiently provide improvement in the absorbability of the drug without being affected by the amount and quality of a meal. | 10-28-2010 |
20100280091 | TRI-SUBSTITUTED 2-BENZHYDRYL-5-BENZYLAMINO-TETRAHYDRO-PYRAN-4-OL AND 6-BENZHYDRYL-4-BENZYLAMINO-TETRAHYDRO-PYRAN-3-OL ANALOGUES, AND NOVEL 3,6-DISBUSTITUTED PYRAN DERIVATIVES - Novel 3,6-disubstituted pyrans, optionally with a further substituent at the 4-position, are monoamine reuptake inhibitors with activity profiles of anti-depressants. | 11-04-2010 |
20100292290 | NOVEL PROCESS TO PREPARE ALMOTRIPTAN - The present invention relates to a novel process for the preparation of almotriptan and pharmaceutically acceptable salts thereof, which affords product conveniently and efficiently with commercially acceptable yields and purity. The present invention also relates to a novel synthetic intermediate used in the process. | 11-18-2010 |
20100305182 | COMPOUNDS AND METHODS FOR MODULATING COMMUNICATION AND VIRULENCE IN QUORUM SENSING BACTERIA - The present invention provides compositions and methods for modulating the communication and virulence of quorum sensing bacteria. In various exemplary embodiments, the invention provides a combinatorial library of quorum sensing compounds including synthetic analogs of naturally occurring and non-naturally occurring acyl-homoserine lactone (AHL) analogs, and methods of synthesizing and using these compounds. | 12-02-2010 |
20100317709 | SPHINGOSINE-1-PHOSPHATE (S1P) RECEPTOR COMPOUNDS - The invention relates to compounds, in particular 2-amino-3,4,5,-trisubstituted thiophenes, pharmaceutical compositions containing them and the uses of said compounds and compositions for diseases related to sphingosine-1-phosphate (S1P) receptors, predominantly S1P3 receptors. The diseases include cardiovascular diseases, atherosclerosis, cancer, pulmonary oedema, autoimmune disorders and Adult Respiratory Distress Syndrome. | 12-16-2010 |
20110003877 | SMAC Mimetic - A SMAC mimetic and pharmaceutical compositions thereof and methods of use. | 01-06-2011 |
20110071206 | Modulators of ATP-Binding Cassette Transporters - Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention. | 03-24-2011 |
20110086900 | COMPOSITIONS FOR PREVENTION/PROPHYLACTIC TREATMENT OF POISON IVY DERMATITIS - The present invention, in one or more embodiments, comprises water-soluble derivatives of 3-n-pentadecylcatechol (poison ivy urushiol saturated congener) and/or 3-n-heptadecylcatechol (poison oak urushiol saturated congener) as compositions for the prevention and/or prophylactic treatment of contact dermatitis caused by poison ivy and poison oak. The present invention is also directed towards processes for making such compounds. Disclosed are compounds which are effective for tolerizing and desensitizing a subject against allergens contained in plants of the Anacardiaceae and Ginkgoaceae families comprising water soluble urushiol esters of general formula (I) Tolerizing and desensitizing mammals, including humans, to allergens contained in plants of the Anacardiaceae and Ginkgoaceae families is attained by administering a composition containing at least one water soluble urushiol ester compound. | 04-14-2011 |
20110105580 | NOVEL POLYMORPHIC FORMS OF SUNITINIB BASE - The present invention relates to novel polymorphic forms of N-[2-(diethylamino)ethyl]-5-[(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl-2,4-dimethyl-1H-pyrrole-3-carboxamide-Sunitinib base (I). The present invention also relates to methods of preparing such polymorphic crystals. | 05-05-2011 |
20110112164 | NOVEL POLYMORPHS AND PROCESSES FOR THEIR PREPARATION - The present invention relates to novel polymorph forms III and IV of sunitinib malate, pharmaceutical compositions comprising the novel polymorphs and the use of the pharmaceutical compositions. The present invention further relates to processes for the preparation of polymorph form I, III and IV of sunitinib malate. | 05-12-2011 |
20110124700 | SYSTEMS AND METHODS OF CANCER STAGING AND TREATMENT - Methods of assessing the sensitivity of a cancer cell to a tyrosine kinase inhibitor are disclosed. Such methods include assessing the expression of miR-497 and correlating reduced expression with sensitivity to the tyrosine kinase inhibitor. Also disclosed are methods of assessing the sensitivity of a cell to a tyrosine kinase inhibitor that includes assessing the expression of FGF1, HOXC10, and/or LHFP. Additionally disclosed are methods of treating patients with tyrosine kinase inhibitors such as sunitinib based on results obtained from the disclosed methods and kits that facilitate the methods. | 05-26-2011 |
20110144179 | Substituted Heterocyclic Mercaptosulfonamide Metalloprotease Inhibitors - The present invention generally relates to substituted heterocyclic mercaptosulfonamide compounds, precursors, and derivatives as well as methods for the preparation of and pharmaceutical compositions comprising these compounds. These compounds are designed to be potent selective inhibitors of matrix metalloproteinases (MMPs), including, for example, gelatinases, collagenases, matrilysins, metalloelastase, stromelysin, and membrane-type 1 matrix metalloproteinase. These inhibitors may be used for the control of physiological and pathological processes and disease conditions in which MMPs are believed to play significant functions. | 06-16-2011 |
20110160272 | METHODS AND COMPOSITIONS FOR USE OF ANGIOGENESIS INHIBITORS IN THE PREVENTION AND/OR CONTROL OF EPILEPSY - In accordance with some preferred embodiments, without limitation, the invention comprises methods and compositions for the prophylactic and/or antiepileptic administration of angiogenesis inhibitors in conjunction with seizures or traumatic insults to the brain, which administration may limit the extent of trauma-associated angiogenesis and/or decrease the likelihood that angiogenesis will give rise to regional epileptogenecity by preventing/reducing the associated increases in blood-brain barrier permeability among new or existing blood vessels along with their epileptogenic effects. | 06-30-2011 |
20110190366 | SUBSTITUTED 2-INDOLINONE AS PTK INHIBITORS CONTAINING A ZINC BINDING MOIETY - The present invention relates to substituted 2-indolinone containing zinc-binding moiety based derivatives that have enhanced or unique properties as inhibitors of protein tyrosine kinase (PTK) receptors and their use in the treatment of PTK related diseases and disorders such as cancer. The said derivatives may further act as HDAC inhibitors. | 08-04-2011 |
20110230538 | PHARMACEUTICAL FOR USE IN THE TREATMENT OF URETEROLITHIASIS - The present invention provides pharmaceutical compositions useful for relieving pain caused by ureteral calculi, facilitating exclusion of ureteral calculi or the like. That is, the present invention provides a pharmaceutical composition for the treatment of ureteral lithiasis, which comprises as an active ingredient an indoline derivative represented by the following general formula (I) or a salt thereof. In the formula, R represents saturated or unsaturated aliphatic acyl which may have a substituent; hydroxyalkyl; aliphatic acyloxyalkyl; lower alkyl which has as a substituent lower alkoxy, carboxy, lower alkoxycarbonyl, aryl-substituted lower alkoxycarbonyl, carbamoyl, mono or di (lower alkyl)-substituted carbamoyl or cyano; optionally substituted aromatic acyl; furoyl or pyridylcarbonyl; R | 09-22-2011 |
20110251253 | SOLID FORMS OF (R)-1-(2,2-DIFLUOROBENZO[D][1,3]DIOXOL-5-YL)-N-(1-(2,3-DIHYDROXYPROPYL)-6- -FLUORO-2-(1-HYDROXY-2-METHYLPROPAN-2-YL)-1H-INDOL-5-YL) CYCLOPROPANECARBOXAMIDE - The present invention relates to solid forms of (R)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide (Compound 1) in substantially crystalline form (Form A) or amorphous form, pharmaceutical compositions thereof, and methods of treatment therewith. | 10-13-2011 |
20110257237 | PROCESS FOR THE PREPARATION OF CRYSTALLINE FORMS OF SUNITINIB MALATE - The present invention, relates to novel processes for the preparation of sunitinib malate formula (I), pharmaceutical compositions comprising said polymorph and the use of the said pharmaceutical compositions in the treatment of various forms of cancer. | 10-20-2011 |
20110257238 | Heteroaryl Dihydroindolones as Kinase Inhibitors - The present invention provides a compound represented by the formula: | 10-20-2011 |
20110263670 | NOVEL POLYMORPHS OF SUNITINIB AND PROCESSES FOR THEIR PREPARATION - The present invention relates to novel polymorphs of sunitinib free base designated form II and form III and to processes for their preparation. The invention also relates to their use as APIs and in the preparation of various forms of sunitinib. Further, the invention relates to pharmaceutical compositions comprising said novel polymorphs and salts, solvates and hydrates prepared according to the invention, and to the uses of said pharmaceutical compositions in the treatment and/or prevention of cancer. | 10-27-2011 |
20110275689 | Preparation of 3-Pyrrole Substituted 2-Indolinone Derivatives - The present invention relates to novel intermediates and further to the use of said intermediates in processes for the preparation of indolinone derivatives, in particular 3-pyrrole substituted 2-indolinones having amide moieties on the pyrrole ring. Such compounds are useful in die treatment of abnormal cell growth, such as cancer, in mammals. | 11-10-2011 |
20110275690 | NEW CRYSTAL FORM OF SUNITINIB MALATE - A process for the preparation of a new crystal form of sunitinib malate, along with pharmaceuticals comprising the same are described. | 11-10-2011 |
20110288143 | BLADDER CANCER TREATMENT AND METHODS - Therapeutic compositions comprising an indoloquinone compound and various bladder cancer treatments and methods are disclosed. More specifically, the compositions comprise an indoloquinone compound and a formulation vehicle. The formulation vehicle improves the solubility and stability of the indoloquinone compound. Additionally, the coating compositions can include coating agents that provide better adhesion of the coating composition to the bladder wall during intravesical delivery of the coating composition. | 11-24-2011 |
20110301216 | ANTICANCER AND ANTIMICROBIAL COMPOUNDS FROM ANTARCTIC EXTREMOPHILIC MICROORGANSIMS - The present disclosure describes the isolation of extremophilic microorganisms from the Lakes of Schirmacher Oasis located in the East Antarctic Dronning Maud Land. The isolated organisms were characterized and certain pigments produced by these microorganisms were isolated. The present disclosure teaches that the isolated pigments exhibit anticancer and antimicrobial properties and can be used as new therapies for the treatment and prevention of cancer and microbially-mediated diseases. | 12-08-2011 |
20110306647 | NOVEL POLYMORPHS OF SUNITINIB MALATE - The present invention provides a novel crystalline form of sunitinib malate, process for its preparation and to pharmaceutical composition containing it. The present invention also provides a process for preparation of sunitinib malate crystal form I. Thus, for example, sunitinib malate was added to water, the mixture was heated to 80 deg C. to obtain a clear solution and stirred for 30 minutes at 80 deg C., slowly cooled to room temperature and the solution was subjected to freeze drying at about −90 deg C. for 8 hours to give sunitinib malate crystalline form III. | 12-15-2011 |
20110319463 | PREVENTIVE OR THERAPEUTIC AGENTS FOR OPTIC NERVE DISORDERS COMPRISING 4,6-DICHLORO-1H-INDOLE-2-CARBOXYLIC ACID DERIVATIVES OR SALTS THEREOF AS ACTIVE INGREDIENTS - A method for preventing or treating an optic nerve disorder, inhibiting retinal nerve cell death or recovering a neurofilament light chain expression level by administering to a patient a pharmacologically effective amount of at least one of the compound represented by the following formula (1): | 12-29-2011 |
20120015999 | FORMULATIONS OF (R)-1-(2,2-DIFLUOROBENZO[D] [1,3] DIOXOL-5-YL)-N-(1-(2,3-DIHYDROXYPROPYL)-6-FLUORO-2-(1-HYDROXY-2-METHYLPRO- PAN-2-YL)-1H-INDOL-5-YL)CYCLOPROPANECARBOXAMIDE - The present invention relates to formulations of (R)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide (Compound 1), pharmaceutical packs or kits thereof, and methods of treatment therewith. | 01-19-2012 |
20120029046 | CRYSTALLINE FORM OF SUNITINIB AND PROCESSES FOR ITS PREPARATION - The present invention relates to a novel crystalline form of sunitinib free base designated form I and to processes for its preparation. The invention also relates to its use as an API and in the preparation of various forms of sunitinib. Further, the invention relates to pharmaceutical compositions comprising the novel crystalline form and salts, solvates and hydrates prepared according to the invention, and to the uses of said pharmaceutical compositions in the treatment and/or prevention of cancer. | 02-02-2012 |
20120046330 | PHARMACEUTICAL COMPOSITIONS OF (R)-1-(2,2-DIFLUOROBENZO[D] [1,3]DIOXOL-5-YL)-N-(1-(2,3-DIHYDROXYPROPYL)-6-FLUORO-2-(1-HYDROXY-2-METH- YLPROPAN-2-YL)-1H-INDOL-5-YL) CYCLOPROPANECARBOXAMIDE AND ADMINISTRATION THEREOF - A pharmaceutical composition comprising Compound 1, (R)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide, and at least one excipient selected from: a filler, a diluent, a disintegrant, a surfactant, a glidant and a lubricant, the composition being suitable for oral administration to a patient in need thereof to treat a CFTR mediated disease such as Cystic Fibrosis. Methods for treating a patient in need thereof include administering the pharmaceutical composition of Compound 1 are also disclosed. | 02-23-2012 |
20120077859 | C-substituted Diindolylmethane Compositions and Methods for the Treatment of Multiple Cancers - The present embodiment of the invention is generally directed to compositions comprising suspensions of poorly water soluble compounds recrystallized in nanoparticulate sizes ranging from 0.1 to 5 μm. In addition, the embodiment of the invention is directed to methods for preparation and administration of these compositions to a patient for prevention and treatment of disease states. In particular, the embodiment of the invention is directed to compositions comprising suspensions of poorly water-soluble compounds, such as antimitotics and antibiotics, in nanoparticulates and methods of prevention and treatment of chronic disease states, such as cancer, by intraperitoneal and intravenous administration of such compositions. | 03-29-2012 |
20120101143 | Compounds Having Activity in Increasing Ion Transport by Mutant-CFTR and Uses Thereof - The invention provides compositions, pharmaceutical preparations and methods for increasing activity (e.g., ion transport) of the mutant cystic fibrosis transmembrane conductance regulator protein (mutant-CFTR), e.g., DF508 CFTR, G551D-CFTR, G1349D-CFTR, or D1152H-CFTR, that are useful for the treatment of cystic fibrosis (CF). The compositions and pharmaceutical preparations of the invention may comprise one or more phenylglycine-containing compounds or sulfonamide-containing compounds of the invention, or an analog or derivative thereof. | 04-26-2012 |
20120115922 | SMAC MIMETEC - A SMAC mimetic and pharmaceutical compositions thereof and methods of use. | 05-10-2012 |
20120122948 | 3-ALKYL-5-FLUOROINDOLE DERIVATIVES AS MYELOPEROXIDASE INHIBITORS - The invention relates to a compound of formula (Ia) | 05-17-2012 |
20120142749 | SOLID SALT FORMS OF A PYRROLE SUBSTITUTED 2-INDOLINONE - The present invention relates to solid salt forms of the 3-pyrrole substituted 2-indolinone compound 5-[5-fluoro-2-oxo-1, 2-dihydro-indol-(3Z)-ylidenemethyl]-2,4-dimethyl-1H-pyrrole-3-carboxylic acid (2-pirrolidin-1-yl-ethyl)-amide. It also relates to polymorphs of the phosphate salt of the amide. The invention further relates to the use of the salts and polymorphs in the treatment of protein kinase related disorders. | 06-07-2012 |
20120232123 | LIQUID PHARMACEUTICAL COMPOSITIONS - Aqueous liquid pharmaceutical composition comprising a) almotriptan and b) at least one compound selected from i) 1′-methyl-5-((pyrrolidin-1-ylsulfonyl)methyl)spiro[indoline-3,3′-pyrrolidin]-2-ol, and ii) 3-(2-(dimethylamino)ethyl)-5-((pyrrolidin-1-ylsulfonyl)methyl)-1H-indol-2-ol. | 09-13-2012 |
20120252860 | Novel N, N'-Hydrazino-bis-isatin Derivatives with Selective Activity Against Multidrug-Resistant Cancer Cells - The invention is directed to a compound of Formula (I), | 10-04-2012 |
20120252861 | Medical Compositions for Intravesical Treatment of Bladder Cancer - Anti-cancer coating compositions comprising 3-hydroxymethyl-5-aziridinyl-1-1-methyl-2-[1H-indole-4,7-dione]propenol (E09) are disclosed. More specifically, the coating compositions comprise EO9 and a formulation vehicle. The formulation vehicle improves the solubility and stability of EO9. Additionally, the coating compositions can include coating agents that provide better adhesion of the coating composition to the bladder wall during intravesical delivery of the coating composition. | 10-04-2012 |
20120258995 | New Indolinone Protein Kinase Inhibitors - The present invention relates to new indolinone compounds and their pharmaceutically acceptable salts and prodrugs for treating and preventing VEGFR related cellular disorders such as cancer. | 10-11-2012 |
20120264803 | METHOD FOR PREDICTING THERAPEUTIC EFFECTS OF CHEMOTHERAPY ON HEPATOCELLULAR CARCINOMA PATIENTS - The present invention provides a method for predicting therapeutic effects of chemotherapy on hepatocellular carcinoma patients who have been treated with transarterial embolization and an antitumor agent for treating cancer patients who have been predicted to have a high probability of obtaining sufficient therapeutic effects from such chemotherapy. The present invention also provides a method for predicting therapeutic effects of chemotherapy on hepatocellular carcinoma patients who have been treated with transarterial embolization using the expression level of PDGF-BB or IL-8 as an indicator and an antitumor agent for treating cancer patients who have been predicted to have a high probability of obtaining therapeutic effects by such prediction method. | 10-18-2012 |
20120289571 | POLYMERIC CONJUGATES OF AROMATIC AMINE CONTAINING COMPOUNDS INCLUDING RELEASABLE UREA LINKER - The present invention relates to releasable urea linker systems involving amine-containing chemical compounds and biologically active agents. In particular, the present invention relates to reversibly releasable linkers based on intramolecular cyclization-assisted releasable urea linkages to aromatic amine-containing compounds. The present invention also relates to polymeric conjugates of indolinone-based tyrosine kinase inhibitors. | 11-15-2012 |
20120289572 | Nicotinic Acetylcholine Receptor Sub-Type Selective Amides of Diazabicycloalkanes - Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are amide compounds which can be prepared from certain heteroaryl carboxylic acids and certain diazabicycloalkanes. The compounds exhibit selectivity for, and bind with high affinity to, neuronal nicotinic receptors of the α4β2 subtype in the central nervous system (CNS). The compounds and compositions can be used to treat and/or prevent a wide variety of conditions or disorders, particularly CNS disorders. The compounds can: (i) alter the number of nicotinic cholinergic receptors of the brain of the patient, (ii) exhibit neuroprotective effects, and (iii) when employed in effective amounts, not result in appreciable adverse side effects (e.g. side effects such as significant increases in blood pressure and heart rate, significant negative effects upon the gastrointestinal tract, and significant effects upon skeletal muscle). | 11-15-2012 |
20120295948 | INDIRUBIN-3'-OXIME DERIVATIVES AS POTENT CYCLIN DEPENDENT KINASE INHIBITORS - The present invention relates to an indirubin-3′-oxime derivative as potent cyclin dependent kinase inhibitor with anti-cancer activity. More particularly, this invention relates to an indirubin-3′-oxime derivative as potent cyclin dependent kinase inhibitor having excellent anti-cancer activity against human lung cancer cell, human fibro sarcoma cell, human colon cancer cell, human leukemia cell, human stomach cancer cell, human nasopharyngeal cancer cell and/or human breast cancer cell. | 11-22-2012 |
20120302620 | NOVEL PYRONE-INDOLE DERIVATIVES AND PROCESS FOR THEIR PREPARATION - The present invention relates to a method for treating a variety of maladies and conditions; which comprises administering a formulation comprising an effective amount of a pyrone-indole derivative of formula (I): | 11-29-2012 |
20120309807 | METHODS AND COMPOSITIONS RELATED TO REGULATION OF CYTOKINE PRODUCTION BY GLYCOGEN SYNTHASE KINASE 3 (GSK-3) - This invention relates generally to a method of treating inflammation and associated diseases and disorders by administering an agent that inhibits glycogen synthase kinase 3 activity. | 12-06-2012 |
20120309808 | COMPOSITIONS AND METHODS FOR EPIGENETIC MODIFICATION OF NUCLEIC ACID SEQUENCES - Provided herein are pharmaceutical compositions and methods for treating disorders characterized by reduced expression of anti-oxidative stress enzymes in a subject. In one aspect, the present invention provides a method for inducing expression of anti-oxidative stress enzymes in a subject in need thereof. The method includes administering to the subject a therapeutically effective amount of a demethylating agent. The demethylating agent includes a phytochemical that induces expression of Nrf2 and Nrf2-mediated genes expressing anti-oxidative stress. Such phytochemicals include indoles, such as 3,3′-diindolylmethane (DIM) and indole-3-carbinol (I3C), and isothiocyanates, such as phenethyl isothiocyanate (PEITC) and sulforaphane (SFN). | 12-06-2012 |
20120322844 | SUBSTITUTED 2-INDOLINONE AS PTK INHIBITORS CONTAINING A ZINC BINDING MOIETY - The present invention relates to substituted 2-indolinone containing zinc-binding moiety based derivatives that have enhanced or unique properties as inhibitors of protein tyrosine kinase (PTK) receptors and their use in the treatment of PTK related diseases and disorders such as cancer. The said derivatives may further act as HDAC inhibitors. | 12-20-2012 |
20130005789 | Nicotinic Acetylcholine Receptor Sub-Type Selective Amides of Diazabicycloalkanes - Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are amide compounds which can be prepared from certain heteroaryl carboxylic acids and certain diazabicycloalkanes. The compounds exhibit selectivity for, and bind with high affinity to, neuronal nicotinic receptors of the α4β2 subtype in the central nervous system (CNS). The compounds and compositions can be used to treat and/or prevent a wide variety of conditions or disorders, particularly CNS disorders. The compounds can: (i) alter the number of nicotinic cholinergic receptors of the brain of the patient, (ii) exhibit neuroprotective effects, and (iii) when employed in effective amounts, not result in appreciable adverse side effects (e.g. side effects such as significant increases in blood pressure and heart rate, significant negative effects upon the gastrointestinal tract, and significant effects upon skeletal muscle). | 01-03-2013 |
20130012564 | SMAC Mimetic - A SMAC mimetic and pharmaceutical compositions thereof and methods of use. | 01-10-2013 |
20130041008 | COMPOUNDS FOR ENZYME INHIBITION - One aspect of the invention relates to inhibitors that preferentially inhibit immunoproteasome activity over constitutive proteasome activity. In certain embodiments, the invention relates to the treatment of immune related diseases, comprising administering a compound of the invention. In certain embodiments, the invention relates to the treatment of cancer, comprising administering a compound of the invention. | 02-14-2013 |
20130059899 | METHODS OF IDENTIFYING MODULATORS OF GPR17 - The present invention is related to a method of determining a test compound's ability to modify the biological activity of a GPR17. Said method comprises, among others, the step of contacting the test compound with a GPR17, or a functional GPR17 fragment in the presence of a suitable amount of a GPR17 agonist of formula I. | 03-07-2013 |
20130065933 | PHARMACEUTICAL COMPOSITION FOR PERORAL ADMINISTRATION OF DIINDOLYLMETHANE - The invention relates to pharmacy. It comprises block copolymer pharmaceutical compositions containing 3,3′-diindolylmethane (DIM). The pharmaceutical composition for peroral administration comprises 3,3′-diindolylmethane as an active component and a target additive, the target additive being a block copolymer of oxyethylene and oxypropylene, in which the content of the hydrophobic block is less than 50 mass % and the molecular mass of the hydrophilic block is equal to 2,250 Da or more, at a ratio of the active component to the selected block copolymer varying between 10:1 and 2:1. | 03-14-2013 |
20130116298 | ANTITUMOR AGENT OR POSTOPERATIVE ADJUVANT CHEMOTHERAPEUTIC AGENT FOR HEPATOCELLULAR CARCINOMA TREATMENT - The present invention provides an antitumor agent or postoperative adjuvant chemotherapeutic agent for a hepatocellular carcinoma patient who has been treated by transarterial embolization. An antitumor agent or postoperative adjuvant chemotherapeutic agent comprising TSU-68 or a salt thereof, which can be administered to a hepatocellular carcinoma patient within 2 weeks after transarterial embolization, is provided. | 05-09-2013 |
20130131136 | NOVEL METHODS FOR PREDICTING THE RESPONSIVENESS OF A PATIENT AFFECTED WITH A TUMOR TO A TREATMENT WITH A TYROSINE KINASE INHIBITOR - The present invention relates to a method for predicting the responsiveness of a patient affected with a tumor to a treatment with a tyrosine kinase inhibitor such as sunitinib. More specifically, the method of the invention comprises a step of determining the expression level of one marker consisting of the FSHR in a biological sample obtained from said patient, and more specifically in the blood endothelial cells from the tumors. | 05-23-2013 |
20130150422 | COMPOSITIONS AND METHODS FOR TREATMENT OF CYSTIC FIBROSIS AND DISEASES ASSOCIATED WITH ABERRANT PROTEIN CELLULAR PROCESSING - The disclosure relates to resorcylic acid lactones and indolinone-containing compounds for use in treatment of diseases associated with aberrant protein processing, such as cystic fibrosis (CF; mucoviscidosis). The disclosure more generally relates to treatment of aberrant protein processing, such as errors in protein folding, trafficking or post-translational modification. | 06-13-2013 |
20130210885 | CRYSTALLINE FORMS OF L-MALIC ACID SALT OF SUNITINIB - The present invention relates to crystalline forms of L-malic acid salt of sunitinib and its preparation. The crystalline forms of the present invention are designated as Form V and Form VI of L-malic acid salt of sunitinib. Formula (I). | 08-15-2013 |
20130210886 | Novel Derivatives Useful as Antiviral Agents - The invention relates to compounds of formula (I) for use in the prevention and/or treatment of viral infections: Wherein X, Y, Z, T, R | 08-15-2013 |
20130289090 | INDOLE DERIVATIVES AND PROCESS FOR THEIR PREPARATION - Substituted indole derivatives of formula (I) wherein the radicals have e.g. the following meaning: R | 10-31-2013 |
20130296397 | EARLY MARKER OF PROTEINURIA IN PATIENTS TREATED WITH AN ANTI-VEGF TREATMENT - This document provides methods and materials related to determining whether or not a human receiving a therapy (e.g., an anti-VEGF therapy such as a bevacizumab therapy) has developed or is at risk for developing proteinuria. For example, methods and materials for detecting urinary podocytes to determine whether or not a human receiving anti-VEGF therapy has or is at risk for developing proteinuria or kidney injury are provided. | 11-07-2013 |
20130303582 | COMPOSITIONS FOR PREVENTION/PROPHYLACTIC TREATMENT OF POISON IVY DERMATITIS - The present invention, in one or more embodiments, comprises water-soluble derivatives of 3-n-pentadecylcatechol (poison ivy urushiol saturated congener) and/or 3-n-heptadecylcatechol (poison oak urushiol saturated congener) as compositions for the prevention and/or prophylactic treatment of contact dermatitis caused by poison ivy and poison oak. The present invention is also directed towards processes for making such compounds. Disclosed are compounds which are effective for tolerizing and desensitizing a subject against allergens contained in plants of the Anacardiaceae and Ginkgoaceae families comprising water soluble urushiol esters of general formula (I) | 11-14-2013 |
20130317077 | COMPOSITION FOR PREVENTING OR TREATING OBESITY, DYSLIPIDEMIA, FATTY LIVER OR DIABETES CONTAINING INDOLE-3-CARBINOL DERIVATIVE AS ACTIVE INGREDIENT - Disclosed is a composition for preventing or treating obesity, dyslipidemia, fatty liver or diabetes, containing an indole-3-carbinol derivative as an active ingredient. The indole-3-carbinol derivative of the present disclosure can be usefully used as a pharmaceutical or functional food composition for preventing or treating obesity, dyslipidemia, fatty liver or diabetes by inhibiting differentiation of preadipocytes and reducing accumulation of triglyceride in cells. | 11-28-2013 |
20130324583 | METHODS FOR TREATING NEUROLOGICAL DISEASE - Neurological disorders and diseases, such as Alzheimer's disease, Huntington's disease, Parkinson's disease, amyotrophic lateral sclerosis (ALS) and Down's syndrome, can be ameliorated or beneficially treated by administration of a formulation comprising an effective amount of a pyrone-indole derivative of formula (I) | 12-05-2013 |
20130324584 | CATHEPSIN C INHIBITORS - Disclosed are | 12-05-2013 |
20130331425 | POLYMER-SUNITINIB CONJUGATES - The invention relates to (among other things) polymer-sunitinib conjugates and related compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits advantages over sunitinib in unconjugated form. | 12-12-2013 |
20130338208 | FULVENE AND FULVALENE ANALOGS AND THEIR USE IN TREATING CANCERS - Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are fulvene and/or fulvalene analogs. The compounds and compositions can be used to treat and/or prevent a wide variety of cancers, including drug resistant cancers, as well as numerous inflammatory, degenerative and vascular diseases, including various ocular diseases. Representative fulvene and/or fulvalene analogs include fulvene and fulvalene analogues of various dyes, hormones, sugars, peptides, oligonucleotides, amino acids, nucleotides, nucleosides, and polyols. The compounds are believed to function, at least, by inhibiting Nox or ROS. In some embodiments, the Nox is one that is selectively expressed in cancer cells over normal cells, or one that is expressed in higher amounts in cancer cells over normal cells. Thus, the compounds are novel therapeutic agents for a variety of cancers and other diseases. | 12-19-2013 |
20130345281 | CONJUGATED 3-(INDOLYL)- AND 3-(AZAINDOLYL)-4-ARYLMALEIMIDE COMPOUNDS AND THEIR USE IN TUMOR TREATMENT - The present invention relates to 3-(Indolyl)- and 3-(azaindolyl)-4-phenylmaleimide compounds of formula (I) wherein R | 12-26-2013 |
20140011855 | POLYMER-SEMAXANIB MOIETY CONJUGATES - The invention relates to (among other things) polymer-semaxanib moiety conjugates and related compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits advantages over the semaxanib moiety in unconjugated form. | 01-09-2014 |
20140011856 | SALT FORM OF TYROSINE KINASE INHIBITOR - Provided are acid addition salts of (Z)—N-[2-(diethylamino)ethyl]-2-methyl-7-(1,2-dihydro-5-fluoro-2-oxo-3H-indol-3-ylidene)-4,5,6,7-tetrahydro-1H-indol-3-carboxamide, wherein the salt comprising at least one of a number of salts including L-malate, hydrochloride, phosphate, L-tartrate, benzenesulfonate, sulfate, methanesulfonate, succinate, citrate, fumarate, p-toluenesulfonate, hydrobromate, L-mandelate, lactate, acetate or maleate salt. Also provided is a pharmaceutical composition comprising the salt compounds, and a method of treatment by administering a therapeutically effective amount of the salt compounds as preparation of medicaments. | 01-09-2014 |
20140031408 | Biodegradable Intravitreal Tyrosine Kinase Implants - Biocompatible intraocular implants include a tyrosine kinase inhibitor and a biodegradable polymer that is effective to facilitate release of the tyrosine kinase inhibitor into the vitreous of an eye for an extended period of time. The therapeutic agents of the implants may be associated with a biodegradable polymer matrix, such as a matrix that is substantially free of a polyvinyl alcohol. The implants can be placed in an eye to treat or reduce the occurrence of one or more ocular conditions. | 01-30-2014 |
20140039030 | POLYMER-DES-ETHYL SUNITINIB CONJUGATES - The invention relates to (among other things) polymer-des-ethyl sunitinib conjugates and related compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits advantages over des-ethyl sunitinib in unconjugated form. | 02-06-2014 |
20140039031 | PHARMACEUTICAL FORMULATIONS OF ACETYL-11-KETO-B-BOSWELLIC ACID, DIINDOLYLMETHANE, AND CURCUMIN FOR PHARMACEUTICAL APPLICATIONS - The present disclosure is directed to compositions and methods for formulating a pharmaceutical dosage form by forming a composition comprising acetyl-11-keto-β-boswellic acid, diindolylmethane, or curcumin with one or more pharmaceutically acceptable excipients for enhanced solubility to increase bioavailability and improve therapeutic efficacy. The composition can be processed by thermo-kinetic compounding along with conventional methods known in the art, such as hot melt extrusion, melt granulation, compression molding, tablet compression, capsule filling, film-coating, or injection molding. | 02-06-2014 |
20140045910 | NOVEL AMINO-PYRROLINE DERIVATIVES, AND USE THEREOF IN THE PREVENTION AND/OR TREATMENT OF METABOLIC SYNDROME - Novel amino-pyrrolinic derivatives, their pharmacologically acceptable salts and use thereof in the prevention and/or treatment of metabolic syndrome. | 02-13-2014 |
20140073680 | BLADDER CANCER TREATMENT AND METHODS - Therapeutic compositions comprising an indoloquinone compound and various bladder cancer treatments and methods are disclosed. More specifically, the compositions comprise an indoloquinone compound and a formulation vehicle. The formulation vehicle improves the solubility and stability of the indoloquinone compound. Additionally, the coating compositions can include coating agents that provide better adhesion of the coating composition to the bladder wall during intravesical delivery of the coating composition. | 03-13-2014 |
20140094499 | FORMULATIONS OF (R)-1-(2,2-DIFLUOROBENZO[D] [1,3] DIOXOL-5-YL)-N-(1-(2,3-DIHYDROXYPROPYL)-6-FLUORO-2-(1-HYDROXY-2-METHYLPRO- PAN-2-YL)-1H-INDOL-5-YL)CYCLOPROPANECARBOXAMIDE - The present invention relates to formulations of (R)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide (Compound 1), pharmaceutical packs or kits thereof, and methods of treatment therewith. | 04-03-2014 |
20140200253 | INDIRUBIN DERIVATIVE HAVING HIGHLY SELECTIVE CYTOTOXICITY FOR MALIGNANT TUMORS - An agent for treating malignant tumors based on a new mechanism is provided, which comprises an indirubin derivative represented by formula (1) or a salt thereof: | 07-17-2014 |
20140249197 | NOVEL INDOLE DERIVATIVES AS SELECTIVE ANDROGEN RECEPTOR MODULATORS (SARMS) - The present invention is directed to novel indole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor. | 09-04-2014 |
20140275201 | IDENTIFICATION OF CANCER STEM CELL MARKERS AND USE OF INHIBITORS THEREOF TO TREAT CANCER - The present invention provides biomarkers of cancer stem cells, as well as cells that have undergone EMT. In addition, the present invention provides methods of treating patients determined to comprise cancer stem cells with PDGFR-β inhibitors to eliminate the cancer stem cells. Methods of predicting sensitivity to PDGFR-β inhibitors, monitoring efficacy of treatment, and determining a prognosis are also provided. | 09-18-2014 |
20140288143 | BLADDER CANCER TREATMENT AND METHODS - Therapeutic compositions comprising an indoloquinone compound and various bladder cancer treatments and methods are disclosed. More specifically, bladder cancer treatments include the intravesical administration of apaziquone immediately following transurethral resection. Also disclosed are therapeutic compositions comprising an indoloquinone compound and a formulation vehicle. The formulation vehicle improves the solubility and stability of the indoloquinone compound. Additionally, the coating compositions can include coating agents that provide better adhesion of the coating composition to the bladder wall during intravesical delivery of the coating composition. | 09-25-2014 |
20140303225 | PHARMACEUTICAL COMPOSITION FOR PERORAL ADMINISTRATION OF 3,3'-DIINDOLYLMETHANE - Block copolymer pharmaceutical compositions containing 3,3′-diindolylmethane (DIM). The pharmaceutical composition for peroral administration comprises 3,3′-diindolylmethane as an active component and a target additive, the target additive being a block copolymer of oxyethylene and oxypropylene, in which the content of the hydrophobic oxypropylene block is less than 50 mass % and the molecular mass of the hydrophilic oxyethylene block is equal to 2,250 Da or more, at a ratio of the active component to the selected block copolymer varying between 1:2 and 1:10. The composition improves absorption of the active compound by the bloodstream upon peroral delivery. | 10-09-2014 |
20140309272 | BIS-INDOLIC DERIVATIVES, A PROCESS FOR PREPARING THE SAME AND THEIR USES AS A DRUG - Novel bis-indolic derivatives, processes for their preparation, and their potential use as new antibacterial drugs. | 10-16-2014 |
20140336234 | CHLOROPHYLL c CONTAINING DEGRANULATION SUPPRESSOR - Degranulation suppressors are provided that are effective against allergic disease and osteoarthritis. The degranulation suppressors contain chlorophyll c. | 11-13-2014 |
20140364476 | CATHEPSIN C INHIBITORS - Disclosed are 4-amino-2-butenamides of Formula (I) having pharmacological activity, pharmaceutical compositions containing them, and methods for the treatment of diseases mediated by the cathepsin C enzyme such as chronic obstructive pulmonary disease. | 12-11-2014 |
20150087687 | COMPOSITIONS AND METHODS TO IMPROVE THE THERAPEUTIC BENEFIT OF INDIRUBIN AND ANALOGS THEREOF, INCLUDING MEISOINDIGO - The present invention describes methods and compositions for improving the therapeutic efficacy of therapeutically active agents previously limited by suboptimal therapeutic performance by either improving efficacy as monotherapy or reducing side effects. Such methods and compositions are particularly applicable to therapeutically active agents selected from the group consisting of: (i) indirubin; (ii) an analog of indirubin; (iii) a derivative of indirubin or of an analog of indirubin; and (iv) a pharmaceutical composition comprising indirubin, an analog of indirubin, or a derivative of indirubin or of an analog of indirubin, especially meisoindigo. | 03-26-2015 |
20150111940 | ASCORBIC ACID SALT OF SUNITINIB - The present invention relates to an ascorbic acid salt of sunitinib and a process for its preparation. The present invention further provides a crystalline Form I of an L-ascorbic acid salt of sunitinib. | 04-23-2015 |
20150119441 | Modulators of ATP-Binding Cassette Transporters - Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention. | 04-30-2015 |
20150361041 | Pyrrole Derivatives as Alpha 7 NACHR Modulators - Disclosed is a compound of formula (I), wherein R | 12-17-2015 |
20160039754 | SYNTHESIS OF DIINDOLYLMETHANES AND INDOLO[3,2-B]CARBAZOLES, COMPOUNDS FORMED THEREBY, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM - Described is a method to make diindolylmethanes and indolyl/pyrrolylmethanes, The method includes the steps of contacting an ether comprising an arylpropargyl moiety and an amine-protected, substituted or unsubstituted aniline moiety with a substituted or unsubstituted indol or a substituted or unsubstituted pyrrole, in the presence of a metal-containing catalyst, for a time and at a temperature to cause an annulation/arylation cascade reaction that yields a diindolylmethane or a indolyl/pyrrolylmethane. The resulting compounds are effective to modulate activity of arylhydrocarbon receptors, to inhibit activity of PCSK9, and to stimulate secretion of glucagon-like peptide 1 in mammals. | 02-11-2016 |
20160051514 | METHODS FOR TREATMENT OF CARDIOMYOPATHY - The methods and assays described herein related to the diagnosis, prognosis and treatment of cardiomyopathy, e.g. arrhythmia. As described herein, the inventors have discovered that certain compounds can be used to treat cardiomyopathies. These compounds are demonstrated herein to reduce expression of nppb, reduce bradycardia, improve contractility, and increase survival. Notably, provided herein is data demonstrating that administration of these compounds can both prevent the development of symptoms when administered prophylactically and reduce symptom severity in subjects where it is administered after the development of symptoms. | 02-25-2016 |
20160096828 | Indole-1-Carboxamides as Kinase Inhibitors - This invention is directed to a compound of Formula I | 04-07-2016 |
20160102077 | Indole-3-Carboxamides as Kinase Inhibitors - This invention is directed to a compound of Formula I | 04-14-2016 |
20160130257 | Macrocyclic proteasome inhibitors - Compositions are provided for selectively inhibiting bacterial proteasome. Also provided are methods for assaying the compositions, methods for treating bacterial infection, and methods for inducing apoptosis in tumor cells using the compositions. | 05-12-2016 |
20160152603 | NITROGEN-CONTAINING HETEROCYCLIC COMPOUND | 06-02-2016 |
20160159778 | NOVEL UREIDO DERIVATIVES OF NAPHTHALENESULFONIC ACIDS - Objects of the present invention are novel ureido derivatives of naphthalensulfonic acids, pharmaceutical compositions comprising such derivatives, a process for the preparation thereof and the use of said derivatives as medications, in particular in the treatment of HIV infections. Formula (I): | 06-09-2016 |
20160166540 | MODULATORS FOR ATP-BINDING CASSETTE TRANSPORTERS | 06-16-2016 |
20180022734 | SUNITINIB PRODRUG AND PHARMACEUTICAL COMPOSITION | 01-25-2018 |
20190142798 | POLYMER-DES-ETHYL SUNITINIB CONJUGATES | 05-16-2019 |