Entries |
Document | Title | Date |
20080207637 | Substituted Pyrazoline Compounds for Reducing Triglycerides in Blood - The present invention relates to substituted pyrazoline compounds, methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animal. | 08-28-2008 |
20080234289 | Melanocortin Receptor-Specific Compounds - A melanocortin receptor-specific compound of the general formula of structure I: | 09-25-2008 |
20080242677 | IMIDAZOLIDINONE DERIVATIVES - The invention is concerned with novel imidazolidinone derivatives of formula (I): | 10-02-2008 |
20080249106 | Novel B1 bradykinin receptor antagonists - The invention encompasses novel compounds and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for treatment of diseases mediated by B1 bradykinin receptor. | 10-09-2008 |
20080300260 | HETEROCYCLIC COMPOUNDS AS POSITIVE MODULATORS OF METABOTROPIC GLUTAMATE RECEPTOR 2 (MGLU2 receptor) - The present invention relates to heterocyclic compounds which are positive modulators of metabotropic glutamate receptor. The present invention also relates to the use of these compounds for preparing a pharmaceutical composition and to a method of treating a medical disorder, selected from neurological and psychiatric disorders associated with glutamate dysfunction. | 12-04-2008 |
20080306089 | PROLINAMIDE-TETRAZOLE DERIVATIVES AS NK3 RECEPTOR ANTAGONISTS - The present invention relates to a compound of formula I | 12-11-2008 |
20090042904 | Substituted Phenly-Piperazine Compounds, Their Preparation And Use In Medicaments - The present invention relates to substituted phenyl-piperazine compounds of general formula (I), a process for their preparation, medicaments comprising said substituted phenyl-piperazine compounds as well as the use of said substituted phenyl-piperazine compounds for the preparation of medicaments, which are particularly suitable for the prophylaxis and/or treatment of disorders or diseases that are at least partially mediated via 5-HT | 02-12-2009 |
20090042905 | TRIAZOLE DERIVATIVES AS LIGANDS OF G-PROTEIN COUPLED RECEPTORS - The present invention provides triazole derivatives according to formula (I) as ligands of G-protein coupled receptors (GPCR), which are useful for the study of and/or the treatment or prophylaxis of physiological and/or pathophysiological conditions in mammals, preferably humans, which are mediated by GPCR. | 02-12-2009 |
20090069340 | Pyrazolone Compounds As Metabotropic Glutamate Receptor Agonists For The Treatment Of Neurological And Psychiatric Disorders - Compounds of Formula (I), wherein R | 03-12-2009 |
20090076028 | DEUTERIUM-ENRICHED ITRACONAZOLE - The present application describes deuterium-enriched itraconazole, pharmaceutically acceptable salt forms thereof, and methods of treating using the same. | 03-19-2009 |
20090111832 | Imidazolidinone Compounds Useful as Beta-Secretase Inhibitors for the Treatment of Alzheimer's Disease - The present invention is directed to imidazolidinone compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved. | 04-30-2009 |
20090118300 | Substituted Imidazole 4-Carboxamides as Cholecystokinin-1 Receptor Modulators - Certain novel substituted imidazole 4-carboxamides are ligands of the human cholecystokinin receptor and, in particular, are selective ligands of the human cholecystokinin-1 receptor (CCK-1R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of CCK-1R, such as obesity, and diabetes. | 05-07-2009 |
20090143405 | MELANIN CONCENTRATING HORMONE RECEPTOR ANTAGONIST - Novel compounds, or pharmaceutically-acceptable salts, tautomers or prodrugs thereof, of Formula I | 06-04-2009 |
20090149472 | SALTS OF SUBSTITUTTED PYRAZOLINE COMPOUNDS, THEIR PREPARATION AND USE AND MEDICAMENTS - The present invention relates to salts of substituted pyrazoline compounds, methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animals. | 06-11-2009 |
20090156612 | Substituted imidazole compound and use thereof - The present invention relates to a compound represented by the formula: | 06-18-2009 |
20090264442 | PYRAZOLE DERIVATIVES AS SIGMA RECEPTOR INHIBITORS - The invention relates to compounds of formula I | 10-22-2009 |
20090275595 | METHOD FOR REDUCTION, STABILIZATION AND PREVENTION OF RUPTURE OF LIPID RICH PLAQUE - There is to provide is an agent for reduction of a lipid rich plaque, stabilization of a lipid rich plaque and/or prevention of rupture of a lipid rich plaque in an atherosclerotic lesion comprising an effective amount of 2-[4-[2-(benzimidazole-2-ylthio)ethyl]piperazin-1-yl]-N-[2,4-bis(methylthio)-6-methyl-3-pyridyl]acetamide (hereinafter, referred to as compound 1), its pharmaceutically acceptable salt or a hydrate thereof and Pitavastatin, and a pharmaceutically acceptable carrier, wherein the agent is intended to be simultaneously administered, or separately administered with interval of time to a patient in need thereof. There is also to provide a method for reduction of a lipid rich plaque, stabilization of a lipid rich plaque and/or prevention of rupture of a lipid rich plaque in an atherosclerotic lesion, comprising simultaneously administering, or separately administering with interval of time an effective amount of the compound 1, its pharmaceutically acceptable salt or a hydrate thereof and an effective amount of Pitavastatin to a patient in need thereof. | 11-05-2009 |
20090318468 | PYRAZOLE COMPOUNDS 436 - There is provided novel compounds of formula (Ia) or (Ib): | 12-24-2009 |
20090325979 | NOVEL IMIDAZOLYLALKYLCARBONYL DERIVATIVES AS CALCIUM CHANNEL MODULATORS AND PREPARATION METHOD THEREOF - Disclosed are novel imidazolylalkylcarbonyl derivatives useful as calcium channel modulators and a preparation method of the same. Also disclosed is a method for the treatment of diseases by administering the above compounds based on their inhibitory activity against calcium channel. | 12-31-2009 |
20100004264 | PYRAZOLE DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO - Pyrazole derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the serotonin 5HT | 01-07-2010 |
20100004265 | 1,2,3-TRIAZOLE DERIVATIVES AS SIGMA RECEPTOR INHIBITORS - The invention relates to compounds having pharmacological activity towards the sigma receptor, and more particularly to 1,2,3-triazole derivatives of formula (I) and to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy and prophylaxis, in particular for the treatment of psychosis or pain. | 01-07-2010 |
20100069400 | METHODS FOR TREATING INFLAMMATION AND RELATED CONDITIONS - A method for treating an inflammatory condition or immune disorder comprises administering to a subject having such a condition or disorder a therapeutically effective amount of at least one compound selected from irindalone, physiologically active enantiomers thereof, and pharmaceutically acceptable salts thereof. The invention further provides a method for elevating levels of anti-inflammatory cytokines such as IL-10 and IL-13 while inhibiting expression of pro-inflammatory cytokines. A pharmaceutical composition, useful for example in topical treatment of psoriasis, comprises a therapeutically effective amount of at least one compound selected from irindalone, physiologically active enantiomers thereof, and pharmaceutically acceptable salts thereof, in a vehicle comprising at least one pharmaceutically acceptable excipient, the vehicle being adapted for topical administration to skin of a subject. | 03-18-2010 |
20100130509 | NOVEL ANTIBIOTICS - The invention relates to the field of antibiotic compositions, both inside and outside the medical field. Presented is a new class of antibiotic compounds, variants of bis(1-aryl-5-tetrazolyl)methanes, which are especially useful for combating infections with gram-positive bacteria and especially MRSA. | 05-27-2010 |
20100210665 | DIARYLHYDANTOIN COMPOUNDS - The present invention relates to diarylhydantoin compounds, including diarylthiohydantoins, and methods for synthesizing them and using them in the treatment of hormone refractory prostate cancer. | 08-19-2010 |
20100261732 | 1, 2, 4 -TRIAZOLE DERIVATIVES AS SEROTONERGIC MODULATORS - The invention relates to novel 5-hydroxytryptamine (5-HT) receptor modulator compounds of formula (I); wherein A, B, R | 10-14-2010 |
20100267741 | Compounds, Compositions and Methods Comprising Pyrazole Derivatives - The present invention relates to compounds, compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Tables 1-2 or encompassed by formulas Ia, Ib, IIa, and IIb) or compositions comprising these compounds, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease. | 10-21-2010 |
20100273811 | N-[5-[2-(3,5-Dimethoxyphenyl)ethyl]-1H-pyrazol-3-yl]-4-(3,4-dimethylpipera- zin-1-yl)benzamide and Salts Thereof - There is provided a compound of formula (I): | 10-28-2010 |
20100286166 | COMPOSITIONS FOR THE TREATMENT OF HYPERPHENYLALANINEMIA - The present invention relates to the use of specific types of compounds acting as pharmacological chaperones having a stabilizing activity on the phenylalanine hydroxylase (PAH) enzyme for the prophylaxis and/or treatment of hyperphenylalaninemia (HPA) and phenylketonuria PKU) and diseases, disorders and conditions related thereto. Further, the present invention relates to pharmaceutical compositions containing the compounds according to the present invention as well as to methods of treatment of HPA, in particular, PKU and diseases, disorders and conditions related thereto. | 11-11-2010 |
20100331342 | Immuno Inhibitory Pyrazolone Compounds - Compounds of formula (IA) or (IB) are inhibitors of CD80 and useful in immunomodulation therapy: wherein Ar represents an optionally substituted monocyclic or bicyclic aromatic or heteroaromatic group having from 5 to 10 ring atoms; R | 12-30-2010 |
20100331343 | NOVEL TRIAZOLE DERIVATIVES AS GHRELIN ANALOGUE LIGANDS OF GROWTH HORMONE SECRETAGOGUE RECEPTORS - The present invention provides novel triazole derivatives as ghrelin analogue ligands of growth hormone secretagogue receptors according to formula (I) that are useful in the treatment or prophylaxis of physiological and/or pathophysiological conditions in mammals, preferably humans, that are mediated by GHS receptors. The present invention further provides GHS receptor antagonists and agonists that can be used for modulation of these receptors and are useful for treating above conditions, in particular growth retardation, cachexia, short-, medium- and/or long term regulation of energy balance; short-, medium- and/or long term regulation (stimulation and/or inhibition) of food intake; adipogenesis, adiposity and/or obesity; body weight gain and/or reduction; diabetes, diabetes type I, diabetes type II, tumor cell proliferation; inflammation, inflammatory effects, gastric postoperative ileus, postoperative ileus and/or gastrectomy (ghrelin replacement therapy). | 12-30-2010 |
20110021537 | HETEROCYCLIC PYRAZOLE-CARBOXAMIDESAS P2Y12 ANTAGONISTS - The present invention relates to compounds of the formula I, | 01-27-2011 |
20110021538 | PROCESSES FOR THE PREPARATION OF PYRAZOLE DERIVATIVES USEFUL AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR - The present invention relates to processes for preparing pyrazole derivatives of Formula (I) and salts and pharmaceutical compositions of the salts thereof, useful as modulators of 5-HT | 01-27-2011 |
20110136824 | UROTENSIN II RECEPTOR ANTAGONISTS - The invention is directed to Urotensin II antagonists. More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating Urotensin-II mediated disorders. Pharmaceutical and veterinary compositions and methods of treating cardiovascular disorders and various other disease states or conditions using compounds of the invention are also described. | 06-09-2011 |
20110152288 | METHODS OF TREATING VASOMOTOR SYMPTOMS - The present invention relates to methods for treating, preventing or controlling vasomotor symptoms such as hot flashes comprising administering specific norepinephrine/serotonin reuptake inhibitors. | 06-23-2011 |
20110160225 | COMPOSITIONS AND METHODS OF USE FOR TREATING OR PREVENTING LIPID RELATED DISORDERS - Disclosed herein are novel compositions and methods for treating or preventing a variety of disorders and conditions associated with lipid metabolism. The methods generally include administering to a patient in need thereof a therapeutically effective amount of a pharmaceutical composition comprising one or more fibric acid or statin derivative compositions alone or in combination with one or more lipid altering agents and/or PDE inhibitors. | 06-30-2011 |
20110201621 | ANGIOTENSIN II RECEPTOR ANTAGONISTS - A compound having the structure | 08-18-2011 |
20110218206 | Individual and combination of mdivi-1 and nutlin-3 for topical or intravitreal ophthalmic use - Disclosed are pharmaceutical compositions comprising mdivi-1 and nutlin-3, individually and in combination, for topical or intravitreal ophthalmic delivery and a method of treatment comprising administering said composition when indicated for glaucoma, optic neuropathies including Leber Hereditary Optic Neuropathy, arteritic or non-arteritic Ischemic Optic Neuropathy, and retinal artery and vein occlusions. | 09-08-2011 |
20120035184 | METHODS FOR INDUCING TUMOR REGRESSION, INHIBITING TUMOR GROWTH, AND INDUCING APOPTOSIS IN BREAST TUMORS WITH GERANYLGERANYLTRANSFERASE I INHIBITORS - Methods of inducing tumor regression, inhibiting tumor growth, and inducing apoptosis with selective peptidomimetic inhibitors of geranylgeranyltransferase I (GGTase I), are provided. In one aspect, GGTI-2418 and its methylester GGTI-2417, increase levels of the cyclin-dependent kinase (Cdk) inhibitor p27 | 02-09-2012 |
20120115880 | Method for Treating Ocular Cancer - Compositions and methods for treating ocular cancer are provided. The composition is a subconjunctival formulation of nutlin-3 and its analogs. The composition provides for methods of treating ocular cancer, including retinoblastoma. The formulation has high penetration into ocular tissue with low toxicity. | 05-10-2012 |
20120142702 | INTEGRIN-LINKED KINASE INHIBITORS - A number of compounds and use of the compounds in a method for treating or preventing cancer in a subject by administering to the subject a pharmaceutical composition including a compound of formula I or a pharmaceutically acceptable salt thereof are described. | 06-07-2012 |
20120232093 | PYRAZOLE DERIVATIVES AS SIGMA RECEPTOR INHIBITORS - The invention relates to compounds of formula I | 09-13-2012 |
20130005739 | PHARMACEUTICAL PREPARATIONS COMPRISING A COS RELEASING COMPOUND - The present invention relates to pharmaceutical compositions comprising a COS releasing compound according to formula (I) and to methods of preparing such compositions. Said pharmaceutical compositions may preferably be used for the treatment and/or the prevention of cardiovascular diseases. | 01-03-2013 |
20130040963 | Compounds, Compositions and Methods of Using Same for Modulating Uric Acid Levels - Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of making and using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid. | 02-14-2013 |
20130040964 | 1,2,3-TRIAZOLE-BASED PEPTIDOMIMETIC INTEGRIN INHIBITORS FOR THE DIAGNOSIS AND THERAPY OF TUMORS - The present invention refers to the field of chemical compounds bearing a 1,2,3-triazole ring of formula (I) and possessing guanidino and carboxylic groups or their isosteres, their preparation by Cu-catalyzed “click-chemistry”, and medical-diagnostic use in pathologies where angiogenesis is altered, for example pathologic conditions of tumor origin, tumor metastasis, osteoporosis, and rheumatoid arthritis. | 02-14-2013 |
20130059860 | NAPHTHALENE CARBOXAMIDE M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS - The present invention is directed to naphthalene carboxamide compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimers disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor. | 03-07-2013 |
20130079355 | Use of Flibanserin in the Treatment of Obesity - The invention relates to a method for the treatment of obesity and related diseases comprising the administration of a therapeutically effective amount of Flibanserin. | 03-28-2013 |
20130225603 | MDM2 INHIBITORS FOR TREATMENT OF OCULAR CONDITIONS - Provided herein are pharmaceutical compositions for the treatment of various ocular diseases characterized by unwanted cellular proliferation. The pharmaceutical compositions may comprise one or more MDM2 inhibitors, and may further comprise one or more additional therapeutic agents. Also provided are methods of use of MDM2 inhibitors and/or formulations thereof for the treatment of ocular diseases characterized by unwanted cellular proliferation. | 08-29-2013 |
20130245039 | COMBINATION THERAPY FOR PROLIFERATIVE DISORDERS - Treatment of proliferative diseases with a combination of a b-Raf inhibitor and MDM2 inhibitor. | 09-19-2013 |
20130317042 | Method of Treating Ischemia/Reperfusion Injury - An agent for treating ischemia/reperfusion injury, including a therapeutically effective amount of a p53 agonist compound including a cis-imidazoline structure. | 11-28-2013 |
20130324553 | MICROBIOCIDAL PYRAZOLE DERIVATIVES - The present invention provides compounds of formula (I): wherein the substituents are as defined in claim | 12-05-2013 |
20130331398 | MODULATION OF UBIQUITINATION OF SYNAPTIC PROTEINS FOR THE TREATMENT OF NEURODEGENERATIVE AND PSYCHIATRIC DISORDERS - The instant invention is based, at least in part, on a newly-identified proteasome-independent signaling function of ubiquitinated PSD-95. Mdm2 inhibitors, Mdm4 inhibitors, PSD-95 inhibitors, and/or enantiomers and/or derivatives thereof de-crease endocytosis via preventing PSD-95 ubiquitination, and thereby increase AMPAR, NMDAR, D1 dopamine receptor surface expression in response to a given stimulus (e.g., NMDA, Aβ). Accordingly, the invention provides methods for modulating AM-PARS, NMDARs, or D1 dopamine receptors in a neuronal cell by contacting the neuronal cell with an Mdm2 and/or Mdm4 inhibitor or PSD-95 inhibitor and/or enantiomers and/or derivatives thereof. Mdm2 and/or Mdm4 inhibitors decrease the enzymatic activity of the respective proteins, and/or interactions with their respective substrates. Mdm2 and Mdm4 inhibitors and/or PSD-95 inhibitors of the invention are contemplated for use in the treatment of neurological disorders, neurodevelopmental disorders, and psychiatric disorders. The invention also provides methods to screen for new Mdm2 and Mdm4 inhibitors and PSD-95 inhibitors and/or enantiomers and/or derivatives thereof. | 12-12-2013 |
20130345237 | ARYL-SUBSTITUTED IMIDAZOLES - The compounds of the invention are antagonists of MDM2 and MDMX, with excellent specificity for MDM2 and MDMX over other proteins, and with selective binding affinity to MDMX over MDM2. The compounds can therefore regulate p53 activity and treat a variety of cancers. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. | 12-26-2013 |
20140024657 | SMALL MOLECULE INHIBITORS OF NECROPTOSIS - The invention features a series of heterocyclic derivatives that inhibit tumor necrosis factor alpha (TNF-α) induced necroptosis. The heterocyclic compounds of the invention are described by Formulas (I)-(VIII) and by Compounds (1)-(7), (13)-(26), (27)-(33), (48)-(57), and (58)-(70). These necrostatins are shown to inhibit TNF-α induced necroptosis in FADD-deficient variant of human Jurkat T cells. The invention further features pharmaceutical compositions featuring necrostatins. The compounds and compositions of the invention may also be used to treat disorders where necroptosis is likely to play a substantial role. | 01-23-2014 |
20140066455 | NOVEL COMPOUNDS - There is provided a compound of formula (I): | 03-06-2014 |
20140121218 | METHOD FOR TREATING OCULAR CANCER - It has now been found that the p53 pathway is inactivated in ocular cancers such as retinoblastoma. As such, the present invention is a method for inducing ocular cancer cell death using a p53 activator. In particular embodiments, the p53 activator blocks the interaction between DM2 or DMX and p53. As the p53 activator induces ocular cancer cell death, a method for preventing or treating ocular cancer is also provided. | 05-01-2014 |
20140179712 | PHARMACEUTICAL FORMULATION OF N-[5-[2-(3,5-DIMETHOXYPHENYL)ETHYL]-2H-PYRAZOL-3-YL]-4-[(3R,5S)-3,5-DIMET- HYLPIPERAZIN-1-YL]BENZAMIDE - There are provided pharmaceutical compositions comprising a compound of Formula (I) as defined herein and an amount of an alkaline effervescent agent that is sufficient to provide satisfactory in vitro dissolution; and further comprising one or more pharmaceutically acceptable ingredients; and to processes for obtaining them. | 06-26-2014 |
20140336202 | METHODS OF IDENTIFYING AND USING MDM2 INHIBITORS - Methods of treating subjects with cancer and screening for MDM2 inhibitors that may be effective cancer therapeutics are provided herein. The cancers that may be treated using MDM2 inhibitors using the methods described herein include those that are or may become resistant to treatment with tyrosine kinase inhibitors. Methods of treating subjects with cancers that have, or develop in response to treatment with tyrosine kinase inhibitors, elevated levels of MDM2, Mcl-1 or PP5 or decreased levels of Huwe1 or CAS using MDM2 inhibitors are provided herein. The MDM2 inhibitors may be effective at treating these cancers alone or in combination with a tyrosine kinase inhibitor regardless of p53 status (mutant or wild-type) of the cancer. | 11-13-2014 |
20140371237 | p19Arf, HMGA2 and MDM2 For Use in the Diagnosis and Treatment of Aberrant Cell Growth - Provided are novel methods and compositions for the diagnosis, prognosis and treatment of leiomyomas, in particular uterine leiomyoma (UL). In addition, methods of identifying anti-tumor agents are described. Furthermore, novel methods and compositions are provided for the treatment of diseases characterized by an aberrant growth of mesenchymal stem cells and their descendants and for the treatment of obesity are disclosed. | 12-18-2014 |
20150045372 | PROCESSES FOR THE PREPARATION OF PYRAZOLE DERIVATIVES USEFUL AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR - The present invention relates to processes for preparing pyrazole derivatives of Formula (I) and salts and pharmaceutical compositions of the salts thereof, useful as modulators of 5-HT | 02-12-2015 |
20160009692 | 1-SUBSTITUTED, 4-(SUBSTITUTED PHENOXYMETHYL)-1,2,3-TRIAZOLE COMPOUNDS WITH ANTIFUNGAL PROPERTIES AND METHODS FOR PREPARATION THEREOF | 01-14-2016 |
20160168101 | NOVEL COMPOUNDS | 06-16-2016 |
20160250209 | CANCER TREATMENT WITH COMBINATION OF PLINABULIN AND TAXANE | 09-01-2016 |