Class / Patent application number | Description | Number of patent applications / Date published |
514255030 | Carbocyclic ring bonded directly to the piperazine ring | 79 |
20080214570 | Therapeutic Agents - The present invention relates to compounds of formula I and processes for preparing such compounds, their use in the treatment of obesity, psychiatric and neurological disorders, to methods for their therapeutic use and to pharmaceutical compositions containing them. | 09-04-2008 |
20080214571 | NOVEL COMPOUNDS - Disclosed is a method for use of phenyl sulfone compounds of formula (I) in the treatment of anxiety. | 09-04-2008 |
20080269248 | Tartrate and Malate Salts of Trans-1-((1R,3S)-6-Chloro-3-Phenylindan-1-Yl)-3,3-Dimethylpiperazine - A tartrate and malate salt of trans-1-(6-chloro-3-phenylindan-1-yl)-3,3-dimethylpiperazine, in particular for medical use, pharmaceutical formulations thereof, including for treatment of schizophrenia or other diseases involving psychotic symptoms. | 10-30-2008 |
20080293739 | COMPOUNDS FOR MODULATING T-CELLS - Disclosed are compounds and compositions that modulate T-cells. Such compounds can be used to treat T-cell mediated disease like T-ALL, rheumatoid arthritis, multiple sclerosis, and graft-vs-host disease (GvHD), to name but a few. The compounds have a general structure as shown in Formula I. | 11-27-2008 |
20080300261 | Arylacetic Acids and Related Compounds for Treatment of Alzheimer's Disease - Compounds of formula I | 12-04-2008 |
20090012099 | Novel Compounds - Disclosed is a method for use of phenyl sulfone compounds of formula (I) in the treatment of Alzheimer's disease and age related cognitive decline. | 01-08-2009 |
20090023750 | NOVEL SALTS OF PIPERAZINE COMPOUNDS AS D3/D2 ANTAGONISTS - The present invention relates to novel monohydrochloride, dihydrochloride, monohydrobromide, maleate and methanesulphonate salts of trans 4-{2-[4-(2,3-dichlorophenyl)-piperazine-1-yl]-ethyl}-N,N-dimethylcarbamoyl-cyclohexylamine and/or their hydrates and/or solvates. Moreover, the invention relates to the process for preparing the salts and their hydrates and/or solvates, to their use in the treatment and/or prevention of conditions which require modulation of dopamine receptor and to pharmaceutical compositions containing them. | 01-22-2009 |
20090036468 | PHARMACEUTICAL COMPOSITIONS CONTAINING DOPAMINE RECEPTOR LIGANDS AND METHODS OF TREATMENT USING DOPAMINE RECEPTOR LIGANDS - The present invention relates to pharmaceutical compositions containing dopamine receptor ligands and selective serotonin reuptake inhibitors and to methods of treating disorders such as schizophrenia, major depressive disorder and bipolar depression using combinations of dopamine receptor ligands and selective serotonin reuptake inhibitors. The present invention also relates to methods of treating depression using dopamine receptor ligands. | 02-05-2009 |
20090054461 | PHARMACEUTICAL COMPOSITION COMPRISING A 1-(3-CHLOROPHENYL)-3-ALKYLPIPERAZINE FOR TREATING APETITE DISORDER -
Use of a 1-(3-chlorophenyl)-3-alkylpiperazine of formula (I), in racemic (R, S) form or in the form of the (S) enantiomer, in which R is a linear or branched alkyl group having from 1 to 3 carbon atoms, or of an addition salt thereof with a pharmaceutically acceptable organic or inorganic acid, for treating apetite disorder A pharmaceutical composition that comprises a therapeutically effective amount of a 1-(3-chlorophenyl)-3-alkylpiperazine of formula (I) as previously defined or of an addition salt thereof with a pharmaceutically acceptable organic or inorganic acid, and at least one pharmaceutically acceptable excipient. | 02-26-2009 |
20090088444 | Substituted phenanthrene diketo acids and uses therefor - Provided herein are substituted phenanthrene diketo acid compounds. These compounds comprise the diketo acid moiety on one of carbons C1-C4 and C9 in the phenanthrene ring and at least one further substitutent on the other ring carbons. Also provided are methods of inhibiting an activity of a human immunodeficiency virus (HIV) integrase protein and treating an HIV infection in a subject using the substituted phenanthrene diketo acid compounds. | 04-02-2009 |
20090105275 | PIPERIDINYL AND PIPERAZINYL MODULATORS OF y-SECRETASE - The present invention relates to compounds of Formula I as shown below, wherein the definitions of Het, R | 04-23-2009 |
20090137606 | Chewable formulations - The invention encompasses a solid dose pharmaceutical composition comprising a disagreeable-tasting drug and processes for preparation of the pharmaceutical composition. The pharmaceutical composition is designed not to be swallowed immediately. | 05-28-2009 |
20090156614 | Selective androgen receptor modulators, analogs and derivatives thereof and uses thereof - This invention provides new compounds and uses thereof in treating a variety of diseases or conditions in a subject, including, inter alia, prostate cancer, muscle wasting diseases and/or disorders or a bone-related diseases and/or disorders. | 06-18-2009 |
20090275596 | Treatment of Neurodegenerative Disorders with Thiourea Compounds - A method for treating a neurodegenerative disorder. The method includes administering to a subject in need thereof an effective amount of one or more thiourea compounds of formula (I) or (II): | 11-05-2009 |
20090275597 | METHODS OF TREATING CNS DISORDERS - The present invention relates to methods of treating various CNS disorders, e.g., mania, bipolar disorder and schizophrenia, by administering NMDA receptor antagonists, alone or in combination with dopamine receptor antagonists. | 11-05-2009 |
20090298851 | PHENYL PIPERAZINE COMPOUNDS, PHARMACEUTICAL COMPOSITION COMPRISING THE SAME AND USE THEREOF - The present invention relates to a novel piperazine derivative or pharmaceutically acceptable salt thereof, a process for preparing the same, a pharmaceutical composition for treating central nervous system diseases comprising an effective amount of the piperazine compound and a method of treating central nervous system (CNS) disorder such as psychosis in a mammal. | 12-03-2009 |
20100004266 | Salt or Solvate of 5-Methyl-2(Piperazin-1-Yl)Benzenesulfonic Acid - The present invention provides a novel salt form or solvate of 5-methyl-2-(piperazin-1-yl)benzenesulfonic acid. | 01-07-2010 |
20100004267 | LIQUID PREPARATION - It is provided a liquid preparation stably including (2S)-1-(4-amino-2,3,5-trimethylphenoxy)-3-{4-[4-(4-fluorobenzyl)phenyl]-1-piperazinyl}-2-propanol or its pharmaceutically acceptable salt as an active ingredient. | 01-07-2010 |
20100016334 | PHARMACEUTICAL FORMULATIONS CONTAINING DOPAMINE RECEPTOR LIGANDS - The present invention relates to stable and bioavailable immediate release formulations comprising dopamine receptor ligands. Methods of treating various disorders by administering the formulations are also described. | 01-21-2010 |
20100056545 | NOVEL PHENYLACETATE DERIVATIVES OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF, PREPARATION METHOD THEREOF AND COMPOSITION FOR PREVENTION OR TREATMENT OF DISEASES INDUCED BY ACTIVATION OF T-TYPE CALCIUM ION CHANNEL CONTAINING THE SAME AS AN ACTIVE INGREDIENT - Disclosed herein are a new phenylacetate derivative represented by Chemical Formula 1 or pharmaceutically acceptable salt thereof, a preparation method thereof, and a composition for prevention or treatment of diseases induced by the activation of T-type calcium ion channels containing the same. The composition containing the phenylacetate derivative according to the present invention effectively inhibits the activation of T-type calcium ion channels and may be useful in the prevention or treatment of diseases such as hypertension, cancer, epilepsy, and neurogenic pains induced by the activation of T-type calcium ion channels. | 03-04-2010 |
20100069401 | USE OF CATECHOLAMINES AND RELATED COMPOUNDS AS ANTI-ANGIOGENIC AGENTS - A catecholamine or related compound of formula (I) having (S)-configuration at β-carbon and having a lipophilicity greater than (S)-noradrenalme, a physiologically tolerated salt thereof, a prodrug thereof, a physiologically functional derivative thereof or any mixture thereof is useful as an anti-angiogemc agent A catecholamine or related compound of formula (II) in which a β-hydroxy group has been modified is also anti-angiogemc | 03-18-2010 |
20100105699 | CRYSTALLINE BASE OF TRANS-1-((1R,3S)-6-CHLORO-3-PHENYLINDAN-1-YL)-3,3-DIMETHYLPIPERAZINE - Crystalline base of compound trans-1-(1R,3S)-6-chloro-3-phenylindan-1-yl)-3,3-dimethylpiperazine, processes for the preparation of purified free base or salts of this compound, pharmaceutical compositions comprising the base and medical use thereof, including for treatment of schizophrenia and other psychotic disorders. | 04-29-2010 |
20100137335 | METABOLITES OF (THIO) CARBAMOYL-CYCLOHEXANE DERIVATIVES - The present invention relates to metabolites of (thio)carbamoyl cyclohexane derivatives, particularly, metabolites of trans-4-{2-[4-(2,3-dichlorophenyl)-piperazin-1-yl]-ethyl}-N,N-dimemylcarbamoyl-cyclohexylamine and pharmaceutically acceptable salts thereof, to pharmaceutical compositions containing the same and to their use in the treatment and/or prevention of a conditions which requires modulation of dopamine receptors. | 06-03-2010 |
20100197704 | PHARMACEUTICAL COMPOSITIONS AND METHOD FOR TREATING ACUTE MANIA - The present invention relates to use of (thio)-carbamoyl-cyclohexane derivatives, particularly trans-4-{2-[4-(2,3-dichlorophenyl)-piperazin-1-yl]-ethyl}-N,N-dimethylcarbamoyl-cyclohexylamine and pharmaceutically acceptable salts thereof in the manufacture of a medicament for the treatment of acute mania. Furthermore, the present invention relates to the treatment of acute mania through the administration of (thio)-carbamoyl cyclohexane derivatives, particularly trans-4-{2-[4-(2,3-dichlorophenyl)-piperazin-1-yl]-ethyl}-N,N-dimethylcarbamoyl-cyclohexylamine and pharmaceutically acceptable salts thereof. | 08-05-2010 |
20100227871 | NICOTINIC RECEPTOR AGONISTS FOR THE TREATMENT OF INFLAMMATORY DISEASES - This invention relates to the use of nicotine receptor agonists for treating inflammatory diseases, including a variety of pulmonary diseases. Such agonists have fewer side effects than other anti-inflammatory drugs, such as steroids. Moreover, these agonists can be used alone or in combination with other anti-inflammatory drugs to alleviate pulmonary diseases. | 09-09-2010 |
20100292250 | CRYSTALLINE FORMS OF (S)-7-([1,2,4]TRIAZOLO[1,5-a]PYRIDIN-6-YL)-4-(3,4-DICHLOROPHENYL)-1,2,3,4- - TETRAHYDROISOQUINOLINE AND USE THEREOF - Novel [1,2,4]triazolo[1,5-a]pyridinyl-6-yl-substituted tetrahydroisoquinolines are described in the present invention. These compounds and crystalline forms SA1 and N-2 are used in the treatment of various neurological and physiological disorders. Methods of making these compounds and crystalline forms SA-1 and N-2 are also described in the present invention. | 11-18-2010 |
20110009422 | 1- [2-(2,4-DIMETHYLPHENYLSULFANYL)-PHENYL] PIPERAZINE AS A COMPOUND WITH COMBINED SEROTONIN REUPTAKE, 5-HT3 AND 5-HT1A ACTIVITY FOR THE TREATMENT OF PAIN OR RESIDUAL SYMPTOMS IN DEPRESSION RELATING TO SLEEP AND COGNITION - The use of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine in the treatment of pain and residual symptoms in depression is provided. | 01-13-2011 |
20110009423 | PHENYL-PIPERAZINE DERIVATIVES AS SEROTONIN REUPTAKE INHIBITORS - The invention provides compounds represented by the general formula I | 01-13-2011 |
20110015208 | PHARMACEUTICAL COMPOSITIONS CONTAINING DOPAMINE RECEPTOR LIGANDS AND METHODS OF TREATMENT USING DOPAMINE RECEPTOR LIGANDS - The present invention relates to pharmaceutical compositions containing dopamine receptor ligands and selective serotonin reuptake inhibitors and to methods of treating disorders such as schizophrenia, major depressive disorder and bipolar depression using combinations of dopamine receptor ligands and selective serotonin reuptake inhibitors. The present invention also relates to methods of treating depression using dopamine receptor ligands. | 01-20-2011 |
20110028491 | APOPTOSIS INHIBITOR - It is directed to provide a novel apoptosis inhibitor. Specifically directed is an apoptosis inhibitor containing a biphenylcarboxamide compound represented by the following formula (1) as an active ingredient, wherein R | 02-03-2011 |
20110034479 | Deuterium-enriched alkyl sulfonamides - The present invention is concerned with deuterium-enriched isobutyl and cyclohexylmethyl sulfonamides of formula I and II, and pharmaceutically acceptable salts and methods of use thereof for the treatment of general anxiety disorders, major depressive disorders, attention deficit disorders, attention deficit hyperactivity disorder, Alzheimer's disease, frontotemporal dementia, cognitive impairment associated with age-related dementia, schizophrenia, migraine, sleep disorders, neurodegenerative diseases and obesity. | 02-10-2011 |
20110053957 | MALONATE SALT OF 4-((1R,3S)-6-CHLORO-3-PHENYLINDAN-1-YL)-1,2,2-TRIMETHYLPIPERAZINE AND USES OF SAME - 4-((1R,35)-6-Chloro-3 -phenylindan-1-yl)-1,2,2-trimethylpiperazine hydrogen malonate salt and pharmaceutical comprising and uses of the same, including for the treatment of schizophrenia and other psychotic disorders are described. | 03-03-2011 |
20110144125 | Anti-Arrhythmia Agents, Methods of Their Use, Methods of Their Identification and Kits Therefore - The disclosure describes an animal model for simulating cardiac arrhythmia. Methods of discovering new anti-arrhythmia drugs using the model are described. Novel anti-arrhythmia agents are provided, as are pharmaceutical compositions made from the agents. Methods of inhibiting spontaneous mechanical activity in myocardially-derived biological systems, and methods of treating and preventing cardiac arrhythmia based on novel anti-arrhythmia agents are described. Kits for performing the above methods are also described. | 06-16-2011 |
20110172246 | 1-(2-PHENOXYMETHYLPHENYL)PIPERAZINE COMPOUNDS - The invention relates to compounds of formula I: | 07-14-2011 |
20110178100 | APOPTOSIS INHIBITOR - It is directed to provide a novel apoptosis inhibitor. Specifically directed is an apoptosis inhibitor containing a biphenylcarboxamide compound represented by the following formula (1) as an active ingredient, wherein R | 07-21-2011 |
20110183996 | THE 1-BUTYL-2-HYDROXYARALKYL PIPERAZINE DERIVATIVES AND THE USES AS ANTI-DEPRESSION MEDICINE THEREOF - The invention discloses 1-butyl-2-hydroxyl aralkyl piperazine derivatives and their use as antidepressants. The derivatives of the present invention have triple inhibition effect on the reuptake of 5-HT, NA and DA, and can be administrated to the patients in need thereof in form of composition by route of oral administration, injection and the like. Compared with clinically currently used dual targets antidepressants (such as venlafaxine), said derivatives may have stronger antidepression effect, broader indications, faster onset and lower neurotoxicity and side reaction; and said derivatives have stronger antidepression activity, lower toxicity, higher bioavailability, longer half life and better druggablity, compared with aryl alkanol piperazine derivatives and optical isomers thereof disclosed in prior art. The 1-butyl-2-hydroxyl aralkyl piperazine derivative is the free alkali or its salt of a compound of formula below: | 07-28-2011 |
20110207744 | Method for treating cognitive deficits - The invention relates to methods of treating cognitive dysfunction and improving cognitive functioning comprising the administration of trans-4-((1R,3S)-6-chloro-3-phenylindan-1-yl)-1,2,2-trimethylpiperazine or a pharmaceutically acceptable salt thereof to a patient in need thereof. Moreover the invention relates to an improved binder in a composition comprising 4-((1R,3S)-6-chloro-3-phenylindan-1-yl)-1,2,2-trimethylpiperazine. | 08-25-2011 |
20110218207 | ISOTOPICALLY ENRICHED ARYLSULFONAMIDE CCR3 ANTAGONISTS - Provided herein are isotopically enriched arylsulfonamides, for example, of Formula I, that are useful for modulating CCR3 activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition. | 09-08-2011 |
20110245270 | NICOTINIC RECEPTOR AGONISTS FOR THE TREATMENT OF INFLAMMATORY DISEASES - Use of nicotine receptor agonists for treating inflammatory diseases, including a variety of pulmonary diseases. Such agonists have fewer side effects than other anti-inflammatory drugs, such as steroids. Moreover, these agonists can be used alone or in combination with other anti-inflammatory drugs to alleviate pulmonary diseases. For example, a method of treating pulmonary inflammation of an inflammatory disease selected from the group of asthma, interstitial pulmonary fibrosis (IPF), sarcoidosis, hypersensitivity pneumonitis (HP), and bronchiolitis obliterans with organizing pneumonitis (BOOP) in an animal in need thereof having said inflammation, including administering orally or by inhalation to said animal a nicotinic receptor agonist. | 10-06-2011 |
20120028991 | PHARMACEUTICAL COMPOSITIONS CONTAINING DOPAMINE RECEPTOR LIGANDS AND METHODS OF TREATMENT USING DOPAMINE RECEPTOR LIGANDS - The present invention relates to pharmaceutical compositions containing dopamine receptor ligands and selective serotonin reuptake inhibitors and to methods of treating disorders such as schizophrenia, major depressive disorder and bipolar depression using combinations of dopamine receptor ligands and selective serotonin reuptake inhibitors. The present invention also relates to methods of treating depression using dopamine receptor ligands. | 02-02-2012 |
20120035188 | LIQUID FORMULATIONS OF SALTS OF 1-[2-(2,4-DIMETHYLPHENYLSULFANYL)PHENYL]-PIPERAZINE - Liquid formulations of lactic acid addition salts of 1-[2-(2,4-dimethylphenylsulfanyl)-phenyl]piperazine are provided. | 02-09-2012 |
20120046302 | METHODS OF TREATING CNS DISORDERS - The present invention relates to methods of treating various CNS disorders, e.g., mania, bipolar disorder and schizophrenia, by administering NMDA receptor antagonists, alone or in combination with dopamine receptor antagonists. | 02-23-2012 |
20120196874 | STILBENE ANALOGS AND METHODS OF TREATING CANCER - Stilbene analogs and pharmaceutical compositions that are useful for the treatment of various cancers, including without limitation, colorectal cancer (CRC) and breast cancer are disclosed. The halogenated stilbene analogs include nitrogen heteroaryl groups and/or amino groups on the stilbene ring. | 08-02-2012 |
20120252819 | SOLID DISPERSION FORMULATIONS AND METHODS OF USE THEREOF - The present invention relates to formulations and methods for increasing the bioavailability of 1-(4-benzhydrylpiperazin-1-yl)-3,3-diphenylpropan-1-one, 1-(3,3-diphenylpropanoyl)piperazine, or a salt thereof. In particular, the formulation can include one or more pharmaceutically acceptable matrix polymers to form a solid dispersion, e.g., a spray dried dispersion or a hot melt extrusion. | 10-04-2012 |
20120252820 | METHODS OF TREATING FUNGAL INFECTIONS - Methods of identifying compounds that potentiate the activity of antifungal agents, potentiators identified by these methods, and methods of using potentiators to treat fungal infections are disclosed. | 10-04-2012 |
20120322811 | DEUTERATED 1-PIPERAZINO-3-PHENYL-INDANES FOR TREATMENT OF SCHIZOPHRENIA - The present invention relates to deuterated 1-piperazino-3-phenyl-indanes and salts thereof with activity at dopamine receptors D | 12-20-2012 |
20130040966 | PHARMACEUTICAL FORMULATIONS CONTAINING DOPAMINE RECEPTOR LIGANDS - The present invention relates to stable and bioavailable immediate release formulations comprising dopamine receptor ligands. Methods of treating various disorders by administering the formulations are also described. | 02-14-2013 |
20130059862 | Novel 1, 2-Disubstituted Amido-anthraquinone Derivatives, Preparation Method and application thereof - The invention provides a series of novel 1,2-disubstituted amido-anthraquinone derivatives. Further, the invention also provides the preparation method and application of said derivatives, said application comprises: said derivatives with therapeutically effective amount are prepared into pharmaceutical compositions for inhibition of cancer cell growth, further treating cancer. | 03-07-2013 |
20130109701 | Chemical Compounds | 05-02-2013 |
20130184291 | THERAPEUTIC USES OF 1-[2-(2,4-DIMETHYL-PHENYLSUFLANYL)PHENYL]PIPERAZINE - The invention provides new therapeutic uses of 1-[2-(2,4-dimethyl-phenylsulfanyl)phenyl]-piperazine and pharmaceutically acceptable salts thereof. | 07-18-2013 |
20130231350 | SOLID DISPERSION FORMULATIONS AND METHODS OF USE THEREOF - The present invention relates to formulations and methods for increasing the bioavailability of 1-(4-benzhydrylpiperazin-1-yl)-3,3-diphenylpropan-1-one, 1-(3,3-diphenylpropanoyl)piperazine, or a salt thereof. In particular, the formulation can include one or more pharmaceutically acceptable matrix polymers to form a solid dispersion, e.g., a spray dried dispersion or a hot melt extrusion. | 09-05-2013 |
20130252970 | SULFONYL-SUBSTITUTED BICYCLIC COMPOUNDS AS PPAR MODULATORS FOR THE TREATMENT OF NON-ALCOHOLIC STEATOHEPATITIS - Disclosed herein are new methods of treatment of non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and other fibrotic diseases of the liver in a subject by modulating PPARδ with sulfonyl-substituted bicyclic compounds and compositions as pharmaceuticals. | 09-26-2013 |
20130274270 | POLYMORPHS OF 3-CHLORO-4[(2R)-2-(4-CHLOROPHENYL)-4-[(1R)-1-(4-CYANOPHENYL)ETHYL]-1-PIPE- RAZINYL]-BENZONITRILE, PHARMACEUTICAL COMPOSITIONS AND METHOD OF USE COMPRISING SAID POLYMORPHS, AND A PROCESS FOR PREPARING THEM - Polymorphs of 3-chloro-4[(2R)-2-(4-chlorophenyl)-4-[(1R)-1-(4-cyanophenyl)ethyl]-1-piperazinyl]-benzonitrile are disclosed, as well as pharmaceutical compositions comprising said polymorphs, methods of using the polymorphs, and a process for preparing them. | 10-17-2013 |
20130281462 | ARYL DIAMIDINES AND PRODRUGS THEREOF FOR TREATING MYOTONIC DYSTROPHY - Disclosed herein are compounds (for example, diamidine derivatives and prodrugs) and methods of use thereof, for example in treating muscular dystrophy (DM) or disease caused by a toxic RNA in a subject. In some embodiments, the methods include administering an effective amount of one of more of the disclosed compounds to a subject to treat or inhibit DM or a disease caused by or associated with toxic RNA, such as DM1, DM2, spinocerebellar ataxia type 8 (SCA8), fragile X tremor ataxia syndrome (FXTAS), or Huntington disease-like 2 (HLD2). In some examples, the methods include selecting a subject for treatment, for example selecting a subject with DM1, DM2, SCA8, FXTAS, or HLD2. | 10-24-2013 |
20130289049 | ACID ADDITION SALTS OF THE 2-[2-[[(4-METHOXY-2,6-DIMETHYLPHENYL)SULFONYL]-(METHYL)AMINO]ETHOXY]-N-ME- THYL-N-[3-(4-METHYLPIPERAZIN-1-YL)CYCLOHEXYL] ACETAMIDE AND THE USE THEREOF AS BRADYKININ B1 RECEPTORANTAGONISTS - The present invention relates to the new acid addition salts AB of the following free base of formula A | 10-31-2013 |
20130317043 | Compounds and Methods for Treating Autoimmune Diseases - The invention relates to a compound of Formula I: | 11-28-2013 |
20140051710 | CRYSTALLINE FORM OF CARBAMOYL-CYCLOHEXANE DERIVATIVES - The present invention relates to novel crystalline forms of carbarmoyl-cyclohexane derivatives and, more particularly, to novel co-crystalline forms of trans-1{4-[2-[4-(2,3-dichlorophenyl-piperazin-1-yl]-ethyl]-cyclohexyl}-3,3-dimethly urea hydrochloride and an acid such as fumaric acid. Processes for preparing these forms, compositions containing these forms, and methods of use thereof are also described. | 02-20-2014 |
20140113913 | MCL-1 AS A THERAPEUTIC TARGET IN SCFFBW7 DEFICIENT NEOPLASM - Some embodiments are based on the discovery that proliferative diseases (e.g., neoplastic diseases, for example, tumors or cancers) having an FBW7 mutation or other FBW7 deficiency are sensitive to Mcl1 inhibiting agents, but resistant to pro-apoptotic drugs that do not inhibit Mcl1. Some embodiments provide methods of treating a proliferative disease based on an assessment of FBW7 expression level or mutation status. Some embodiments provide methods of classifying a hyperproliferative cell or cell population, for example, a malignant cell or cell population based on an assessment of FBW7 expression level or mutation status. Some embodiments provide methods of selecting a treatment regimen for treating a proliferative disease, for example, a malignant disorder, based on an assessment of FBW7 expression level or mutation status. | 04-24-2014 |
20140163043 | PHENYL-PIPERAZINE DERIVATIVES AS SEROTONIN REUPTAKE INHIBITORS - The invention provides compounds represented by the general formula I | 06-12-2014 |
20140163044 | Compound Chemical Medicine Acting on Respiratory Disease, Preparation Process and Use Thereof - A pharmaceutical composition for respiratory system disease and the preparation process therefor, consisting of levodropropizine and carbocisteine as active ingredients with a pharmaceutically acceptable excipient. The present pharmaceutical composition has a marked cough-relieving effect and fewer negative reactions. | 06-12-2014 |
20140221395 | Deuterium-Enriched Alkyl Sulfonamides and Uses Thereof - The present invention is concerned with deuterium-enriched sulfonamides of formula 1, their pharmaceutically acceptable salts and methods of use thereof for the treatment of anxiety disorders including, General Anxiety Disorder (GAD), Panic Disorder (PD), Post-Traumatic Stress Disorder (PTSD), Social Phobia (SP), Health Anxiety (Hypochondriasis), depression, major depressive disorders, unipolar depression, bipolar I depression disorder, bipolar II depression disorder, treatment-resistant depression, single episodic and recurrent major depressive disorders, depression in the medically ill, attention deficit hyperactivity disorder (ADHD), attention deficit disorder (ADD), Obsessive-Compulsive Disorder (OCD), Obsessive-Compulsive Personality Disorder (OCPD), Autism Spectrum Disorder (ASD), schizophrenia, psychosis, epilepsy, seizures, hot flashes due to menopause, age-related macular degeneration (AMD), premature ejaculation, male erectile dysfunction, sexual dysfunction, obesity, eating disorders, bulimia nervosa, anorexia nervosa, angina, migraine, pain, nociception, sleep disorders, insomnia, fibromyalgia, alcohol withdrawal, autism, Rett's syndrome, cyclothymic disorder, neural injury, neurodegenerative diseases, Parkinson's disease, Parkinson's disease psychosis, Huntington disease, Alzheimer's disease, frontotemporal dementia, cognitive impairment associated with age-related dementia, Alzheimer's disease, schizophrenia, psychosis, depression, pain or discomfort associated with surgery and pain or discomfort associated with medical illness. | 08-07-2014 |
20140249161 | STILBENE ANALOGS AND METHODS OF TREATING CANCER - Stilbene analogs and pharmaceutical compositions that are useful for the treatment of various cancers, including without limitation, colorectal cancer (CRC) and breast cancer are disclosed. The halogenated stilbene analogs include nitrogen heteroaryl groups and/or amino groups on the stilbene ring. | 09-04-2014 |
20140256743 | CATHEPSIN CYSTEINE PROTEASE INHIBITORS - This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis. | 09-11-2014 |
20140288089 | 1-(2-PHENOXYMETHYLPHENYL)PIPERAZINE COMPOUNDS - The invention relates to compounds of formula I: | 09-25-2014 |
20140315921 | 1-[2-(2,4-Dimethylphenylsulfanyl)-Phenyl]Piperazine As A Compound With Combined Serotonin Reuptake, 5-HT3 And 5-HT1a Activity For The Treatment Of Cognitive Impairment - This disclosure relates to 1-[2-(2,4-dimethylphenylsulfanyl)-phenyl]piperazine or a pharmaceutically acceptable salt thereof in a crystalline form. | 10-23-2014 |
20140364441 | CRYSTALLINE FORMS OF (S)-7-([1,2,4]TRIAZOLO[1,5-a]PYRIDIN-6-YL)-4-(3,4-DICHLOROPHENYL)-1,2,3,4- -TETRAHYDROISOQUINOLINE AND USE THEREOF - Novel [1,2,4]triazolo[1,5-a]pyridinyl-6-yl-substituted tetrahydroisoquinolines are described in the present invention. These compounds and crystalline forms SA1 and N-2 are used in the treatment of various neurological and physiological disorders. Methods of making these compounds and crystalline forms SA-1 and N-2 are also described in the present invention. | 12-11-2014 |
20140378473 | COMPOSITIONS AND METHODS FOR TREATING NEURODEGENERATIVE DISEASE - This invention relates to novel diarylamino compounds that bind to the sigma-2 receptor, to pharmaceutical compositions comprising such compounds, and to methods for inhibiting or restoring synapse loss in neuronal cells, modulating a membrane trafficking change in neuronal cells, and treating cognitive decline and neurodegenerative diseases and disorders therewith. | 12-25-2014 |
20150011566 | N-PHENYLPIPERAZINE DERIVATIVES THAT ARE ANTAGONISTS OF A1A, A1D ADRENOCEPTORS AND 5-HT1A RECEPTORS FOR THE TREATMENT OF BENIGN PROSTATE HYPERPLASIA, PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME - The present invention provides N-phenylpiperazine derivatives for use as multiple binders and/or antagonists of α1A adrenoceptors, α1D adrenoceptors and 5-HT1A serotonin receptors. These substances are candidates to prototypes for the treatment of benign prostate hyperplasia and lower urinary tract symptoms, and are useful in pharmaceutical compositions. | 01-08-2015 |
20150018371 | POSITIVE ALLOSTERIC MODULATORS FOR MELANOCORTIN RECEPTORS - Positive allosteric modulators of melanocortin receptors, especially allosteric potentiators of the receptors MC3R and MC4R are described herein. Also provided are pharmaceutical compositions containing the positive allosteric modulators and methods of treating obesity or an obesity-related disorder such as type 2 diabetes, comprising administering an effective amount of the positive allosteric modulator. | 01-15-2015 |
20150038515 | INHIBITORS OF HEPATITIS B VIRUS CONVALENTLY CLOSED CIRCULAR DNA FORMATION AND THEIR METHOD OF USE - Pharmaceutical compositions of the invention comprise covalently closed circular DNA formation inhibitors having a disease-modifying action in the treatment of diseases associated with the formation of covalently closed circular DNA that include hepatitis B infection, and any disease involving formation of covalently closed circular DNA. | 02-05-2015 |
20150094316 | LIQUID FORMULATIONS OF SALTS OF 1-[2-(2,4-DIMETHYLPHENYLSULFANYL)PHENYL]PIPERAZINE - Liquid formulations of lactic acid addition salts of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine are provided | 04-02-2015 |
20150141437 | AMIDOPHENOXYPROPANOLAMINES - The use of compounds of formula wherein R | 05-21-2015 |
20150297585 | COMPOSITIONS COMPRISING VORTIOXETINE AND DONEPEZIL - Pharmaceutical compositions comprising vortioxetine and donepezil are provided and the use of such composition for the treatment of cognitive dysfunctions. | 10-22-2015 |
20150306094 | TRANS-4--N,N-DIMETHYLCARBAMOYL-CYCLOHEXYLAMINE FOR TREATING NEGATIVE SYMPTOMS OF SCHIZOPHRENIA - The present invention relates to trans-4-{2-[4-(2,3-dichlorophenyl)-piperazin-1-yl]-ethyl}-N,N-dimethylcarbamoyl-cyclohexylamine (cariprazine) and pharmaceutically acceptable salts and hydrates and solvates and polymorphs thereof for use in the treatment of primary negative symptoms of schizophrenia and/or predominantly negative symptoms of schizophrenia. | 10-29-2015 |
20160015706 | CRYSTALLINE FORMS OF AN ANTIDEPRESSANT COMPOUND - The present invention relates to novel crystalline forms of vortioxetine hydrobromide, in particular three crystalline forms, a process for their preparation, a pharmaceutical composition containing said novel crystalline forms, and a process for the purification of vortioxetine or a salt thereof, comprising the formation of one or more of the novel crystalline forms of vortioxetine hydrobromide described herein. | 01-21-2016 |
20160083359 | 1-[2-(2,4-DIMETHYLPHENYLSULFANYL)-PHENYL]PIPERAZINE AS A COMPOUND With COMBINED SEROTONIN REUPTAKE, 5-HT3 AND 5-HT1A ACTIVITY FOR THE TREATMENT OF COGNITIVE IMPAIRMENT - 1-[2-(2,4-dimethylphenylsulphanyl)phenyl]piperazine exhibits potent activity on SERT, 5-HT | 03-24-2016 |
20160108024 | BILATERALLY-SUBSTITUTED TRICYCLIC COMPOUNDS FOR THE TREATMENT OF HUMAN IMMUNODEFICIENCY VIRUS TYPE-1 (HIV-1) INFECTION AND OTHER DISEASES - The invention relates to novel bilaterally-substituted tricyclic compounds and pharmaceutical compositions containing them, for use as medicaments. | 04-21-2016 |
20160158188 | NOVEL USE FOR PAI-1 INHIBITOR - Provided is a novel use of a plasminogen activator inhibitor-1 inhibitor (PAI-1 inhibitor) that is used as an active ingredient of an agent for controlling a tumor stem cell, an agent for enhancing the antitumor effect of an antitumor agent, an agent for tumor chemotherapy, a stem-cell protecting drug, or a hematopoietic disorder improving agent. | 06-09-2016 |
20160200698 | VORTIOXETINE SALT AND CRYSTAL THEREOF, THEIR PREPARATION METHOD, PHARMACEUTICAL COMPOSITIONS AND USAGE | 07-14-2016 |