N.V. Organon Patent applications |
Patent application number | Title | Published |
20130225559 | S-MIRTAZAPINE FOR THE TREATMENT OF HOT FLUSH - The invention provides a method of treatment of hot flush with S-mirtazapine and the use of S-mirtazapine for the manufacture of a medicament for the treatment of hot flush. | 08-29-2013 |
20130023566 | 2-(1,2-BENZISOXAZOL-3-YL)BENZYLAMINE DERIVATIVES - The invention relates to 2-(1,2-benzisoxazol-3-yl)benzylamine derivatives having the general Formula (I) wherein R | 01-24-2013 |
20120309966 | 8-METHYL-1-PHENYL-IMIDAZOL[1,5-A]PYRAZINE COMPOUNDS - The present invention provides 8-methyl-1-phenyl-imidazo[1,5-a]pyrazine deriva-tives according to formula I or pharmaceutically acceptable salts thereof. The compounds of the current invention show inhibitory activity against Lck and can be used for the treatment of Lck-mediated diseases or Lck-mediated conditions such as inflammatory disorders. | 12-06-2012 |
20120245175 | MK2 INHIBITORS - The present invention relates to compounds of general Formula (I) or a pharmaceutically acceptable salt thereof. The compounds can be used in the treatment of immune, autoimmune, inflammatory diseases, cardiovascular diseases, infectious diseases, bone resorption disorders, neurodegenerative diseases or proliferative diseases. | 09-27-2012 |
20120238574 | (1, 1, 1,3,3,3 -HEXAFLUORO-2 HYDROXYPROPAN- 2 -YL) PHENYL DERIVATIVE, PHARMACEUTICAL COMPOSITIONS THEREOF AND THEIR USE FOR THE TREATMENT OF ATHEROSCLEROSIS - The present invention relates to (1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl derivatives having the general formula (I) to pharmaceutical compositions comprising the same and to the use of these (1,1,1,3,3,3-hexafluoro-2-hydroxy-propan-2-yl)phenyl derivatives in the treatment of atherosclerosis. | 09-20-2012 |
20120231497 | SELECTIVE ENZYMATIC HYDROLYSIS OF C-TERMINAL TERT-BUTYL ESTERS OF PEPTIDES - The present invention relates to a process for the selective enzymatic hydrolysis of C-terminal esters of peptide substrates in the synthesis of peptides, comprising hydrolysing C-terminal tert-butyl esters using the protease subtilisin. This process is useful in the production of protected or unprotected peptides. | 09-13-2012 |
20120202996 | TETRAHYDROQUINOLINE DERIVATIVES - The present invention relates to tetrahydroquinoline derivatives having general formula I: | 08-09-2012 |
20120183565 | FULLY HUMAN ANTIBODIES TO BTLA - The present invention relates to binding compounds specific for BTLA and uses thereof. More specifically, the invention relates to fully human antibodies that recognize human BTLA and modulate its activity in cancer, inflammatory, and autoimmune disorders. | 07-19-2012 |
20120107870 | SELECTIVE ENZYMATIC AMIDATION OF C-TERMINAL ESTERS OR ACIDS OF PEPTIDES - The present invention relates to a process for the amidation of C-terminal esters or acids of peptide substrates in solution-phase synthesis of peptides, comprising amidating one or more peptide substrates comprising C-terminal esters or acids using the protease subtilisin in any suitable form in the presence of an ammonium salt derived from an acid having a pKa above 0. | 05-03-2012 |
20120095002 | ISOXAZOLE-5-CARBOXAMIDE DERIVATIVES - The present invention relates to isoxazole-5-carboxamide derivative having the general Formula (I), or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of said isoxazole-5-carboxamide derivatives for the treatment of TRPV1 mediated disorders, such as acute and chronic pain disorders, acute and chronic neuropathic pain, acute and chronic inflammatory pain, respiratory diseases, and lower urinary tract disorders. | 04-19-2012 |
20120039843 | CONJUGATES OF A POLYPEPTIDE AND AN OLIGOSACCHARIDE - The present invention relates to conjugates of a polypeptide and an oligosaccharide, wherein the polypeptide is conjugated to at least one oligosaccharide-spacer residue, the oligosaccharide being a synthetic sulfated oligosaccharide comprising 4-18 monosaccharide units and per se having affinity to antithrombin III and the spacer being a bond or an essentially pharmacologically inactive flexible linking residue, or a pharmaceutically acceptable salt thereof. | 02-16-2012 |
20110224183 | 16, 17-CARBOCYCLIC CONDENSED STEROID COMPOUNDS HAVING SLECTIVE ESTROGENIC ACTIVITY - The invention discloses a steroid compound having the formula (1): | 09-15-2011 |
20110218189 | PYRROLO[2,3-d]PYRIMIDIN-2-YL-AMINE DERIVATIVES AS PKC-THETA INHIBITORS - The present invention relates to a pyrrolo[2,3-d]pyrimidin-2-yl-amine derivative according to formula (I) wherein the variables are defined as in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to a pharmaceutical composition comprising one or more of said pyrrolo[2,3-d]pyrimidine-2-ylamine derivatives and to their use in therapy, for instance in the treatment of PKCθ mediated disorders. | 09-08-2011 |
20110039832 | DIHYDRO)PYRROLO[2,1-A]ISOQUINOLINES - The invention relates to 5,6-dihydropyrrolo[2,1-a]isoquinoline and pyrrolo[2,1-a]isoquinoline derivatives according to general formula (I) or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility. | 02-17-2011 |
20110030681 | DRUG DELIVERY DEVICE - A dispenser for administering a pharmaceutical substance in the form of a plurality of separate unit doses of the substance, comprising a housing, an actuator, a delivery outlet for administering at least one unit dose at a time, a transport mechanism for bringing the unit doses sequentially in operative association with the delivery outlet and a delaying arrangement to impose a lockout interval between administering sequential doses | 02-10-2011 |
20110028451 | Dihydrobenzoindazoles - The invention relates to benzoindazole derivatives according to general Formula I | 02-03-2011 |
20110028450 | Ring-annulated dihydropyrrolo[2,1-alpha]isoquinolines - The invention relates to ring-annulated dihydropyrrolo[2,1-a]isoquinoline compounds according to general Formula I | 02-03-2011 |
20110009428 | NOVEL ANDROGENS - The compounds of the subject invention have a structure according to formula I: | 01-13-2011 |
20110003976 | REMOVAL OF LIPOPOLYSACCHARIDES FROM PROTEIN-LIPOPOLYSACCHARIDE COMPLEXES BY NON FLAMMABLE SOLVENTS - During the production of recombinant proteins from gram negative bacteria, lipopolysaccharides (LPS, endotoxin) are released along with the protein of interest. In many instances, LPS will copurify with the target protein due to specific or non-specific protein-ILPS interactions. We have investigated the ability of alkanediols to effect the separation of LPS from protein-LPS complexes while the complexes are immobilized on anion or cation exchange chromatographic media. Alkanediols provide a safer alternative to the use of other organics such as alcohols or acetonitrile due to their lower toxicity and decreased flammability. In addition, they are less costly than many of the detergents that have been used for such purposes. LPS removal efficiency increased with increasing alkane chain length. 1,2-alkanediols were more effective than terminal alkanediols in the separation of LPS from protein LPS complexes. | 01-06-2011 |
20100331292 | SUBSTITUTED 16,17-ANNELLATED STERIOD COMPOUNDS FOR USE IN WOMENS HEALTHCARE - The present invention relates to substituted steroid compounds having the formula | 12-30-2010 |
20100324021 | (DIHYDRO)IMIDAZOISO[5,1-A]QUINOLINES - The invention relates to imidazoiso[5,1-a]quinoline and 5,6-dihydro-imidazoiso[5,1-a]quinoline derivatives according to general Formula I | 12-23-2010 |
20100267694 | S-MIRTAZAPINE FOR THE TREATMENT OF HOT FLUSH - The invention provides a method of treatment of hot flush with S-mirtazapine and the use of S-mirtazapine for the manufacture of a medicament for the treatment of hot flush. | 10-21-2010 |
20100249083 | 16,17-CARBOCYCLIC CONDENSED STEROID COMPOUNDS HAVING SELECTIVE ESTROGENIC ACTIVITY - The invention discloses a steroid compound having the formula (1): | 09-30-2010 |
20100234618 | Process for the Preparation of Asenapine and Intermediate Products Used in Said Process - The invention relates to a novel process for the preparation of asenapine, i.e. trans-5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenz[2,3:6,7]oxepino[4,5-c]pyrrole, as well as to novel intermediate products for use in said process. | 09-16-2010 |
20100152461 | INTERMEDIATE COMPOUNDS FOR THE PREPARATION OF TRANS-5-CHLORO-2-METHYL-2,3,3A,12B-TETRAHYDRO-1H-DIBENZ[2,3:6,7]-OXEPINO[- 4,5-C]PYRROLE - Disclosed are novel amino acid derivatives of formula (I) and (II) | 06-17-2010 |
20100119445 | PLEXIN D1 AS A TARGET FOR TUMOR DIAGNOSIS AND THERAPY - The present invention relates to plexin D1 for use as a targetable protein in the treatment or diagnosis of disorders that involve expression of plexin D1. Diagnosis is suitably effected by detecting the presence of plexin D1 in the body or a bodily tissue or fluid, whereas treatment is effected by targeting plexin D1 for delivery of therapeutics to the site where treatment is needed. The invention further relates to the use of molecules that bind plexin D1, a nucleic acid encoding plexine D1 or a ligand of plexin D1 for the preparation of a therapeutical composition for the treatment or diagnosis of disorders that involve expression of plexin D1. The disorders comprise disorders in which plexin D1 is expressed on tumor cells, tumor blood vessels or activated macrophages. | 05-13-2010 |
20100104619 | DELIVERY SYSTEM FOR A NON-STEROIDAL NON-IONIZED HYDROPHILIC DRUG - This invention relates to an extended release formulation comprising a solid non-steroidal non-ionized hydrophilic drug, having a molecular weight below 500 Dalton and having a solubility of at least 0.1 wt % in ethylene vinyl acetate copolymer having a vinyl acetate content of 28%, which formulation is a vaginal device having a skin and which device comprises an inner compartment made of a thermoplastic polymer, which polymer is containing the drug. The polymer is preferably made of ethylene-vinyl acetate copolymer. | 04-29-2010 |
20100036126 | STEREOSELECTIVE SYNTHESIS OF (S)-1-METHYL-3-PHENYLPIPERAZINE - This invention provides for a compound according to Formula (1), wherein R | 02-11-2010 |
20100004186 | Antithrombotic Dual Inhibitors Comprising A Biotin Residue - The present invention relates compounds of the formula (I) oligosaccharide-spacer-A (1), wherein the oligosaccharide is a negatively charged oligosaccharide residue comprising two to twenty five monosaccharide units, the charge being compensated by positively charged counterions, and wherein the oligosaccharide residue is derived from an oligosaccharide which has (AT-III mediated) anti-Xa activity per se; the spacer is an essentially pharmacologically inactive flexible linking residue having a chain length of 10 to 70 atoms; A is the residue —CH[NH—SO | 01-07-2010 |
20090306046 | METHOD OF TREATMENT OF HORMONE DEPLETION INDUCED VASOMOTOR SYMPTOMS - The invention provides a method to effectively wean a woman from hormone therapy for treatment of vasomotor symptoms by reducing the dosage of the hormonal agent to zero, while a non-hormonal drug in an amount, which is therapeutically effective for treating vasomotor symptoms, is administered or initiated and continued for a limited period of a duration between 3 and 8 months. | 12-10-2009 |
20090291929 | STEROIDS HAVING A MIXED ANDROGENIC AND PROGESTAGENIC PROFILE - The invention provides for compounds having formula (1) wherein; R | 11-26-2009 |
20090156569 | ORAL CONTRACEPTIVE SPRAY - The subject invention provides a liquid contraceptive formulation for oral transmucosal administration. The formulation comprises etonogestrel, optionally together with ethinyl estradiol but does not contain a matrix former or a percutaneous absorption promoter, which is a hydroxy acid or a salt thereof. | 06-18-2009 |
20090099240 | METHODS FOR TREATING ENERGY METABOLISM DISORDERS BY INHIBITING FATTY ACID AMIDE HYDROLASE ACTIVITY - Disclosed herein are methods for treating energy metabolism disorders by administering a composition containing a therapeutically effective amount of a fatty acid amide hydrolase inhibitor. The composition can also be administered to reduce body fat, body weight, or caloric intake. | 04-16-2009 |
20090062262 | NON STEROIDAL GLUCOCORTICOID RECEPTOR MODULATORS - The present invention relates to compounds having general Formula (I) or a pharmaceutically acceptable salt thereof. In this formula R | 03-05-2009 |
20090030074 | SYNTHESIS, POLYMORPHS, AND PHARMACEUTICAL FORMULATION OF FAAH INHIBITORS - Pharmacological inhibition of fatty acid amide hydrolase (FAAH) activity leads to increased levels of fatty acid amides. The alkylcarbamic acid aryl ester of Formula (I), KDS-4103, is a FAAH inhibitor. Described herein is a process for the preparation of the compound of Formula (I), characterization of polymorphs of the FAAH inhibitor, and their uses therof. | 01-29-2009 |
20090012463 | KIT FOR AND METHOD OF ASSEMBLING AN APPLICATOR FOR INSERTING AN IMPLANT - The invention pertains to a kit for assembling a disposable applicator for inserting an implant, in particular a rod-like implant containing an active substance, under the skin of a human or animal, the kit comprising a first component, in turn comprising a main housing part providing a handle for grasping and maneuvering the applicator, a cannula, and a cannula holder mounted in the main housing part, the main housing part having an opening which allows introduction of an implant into the proximal end of the cannula or the cannula holder, and, a second component for closing said opening, in turn comprising a second housing part and a rod attached to or forming an integral whole with the second housing part and mountable inside the cannula or the cannula holder. | 01-08-2009 |
20090012319 | Process for the preparation 2-substituted-derivatives of estrone and estradiol - The invention provides a process for the preparation of 2-substituted-derivatives of estrone and estradiol. The invention also provides several novel compounds, which can be intermediates in the process, and processes to prepare these novel compounds. The invention also provides 2-alkoxy-estrone, 2-alkoxy-estradiol or mixtures thereof essentially free from other estrogenic intermediates. | 01-08-2009 |
20080280923 | 1-Benzylindole-2-Carboxamide Derivatives - The present invention relates to i-benzylindole-2-carboxamide derivatives of formula I, or a pharmaceutically acceptable salt or solvate thereof. The invention also relates to pharmaceutical compositions comprising said 1-benzylindole-2-carboxamide derivatives and to their use in therapy, particularly for the treatment of obesity or nicotine dependence. | 11-13-2008 |
20080275042 | 4-Phenyl-5-Oxo-1,4,5,6,7,8-Hexahydroquinoline Derivatives for the Treatment of Infertility - The present invention relates to 4-phenyl-5-oxo-1,4)5,6,7,8-hexahydroquinoline derivatives according to Formula I, Formula I or a pharmaceutically acceptable salt thereof, wherein R | 11-06-2008 |
20080262221 | (PYRIDO/THIENO)-[f]-OXAZEPINE-5-ONE DERIVATIVES - The present invention relates to (pyrido/thieno)-[f]-oxazepine-5-one derivatives having the general Formula I | 10-23-2008 |
20080255086 | Heterocyclic Derivatives - The present invention relates to a heterocyclic derivative according to formula I | 10-16-2008 |
20080255074 | Drug Combination Comprising A Selective Serotonin Reuptake Inhibitor And A Glucocorticoid Receptor Antagonist For The Treatment Of Depression - The invention provides for a combination comprising an amount of an SSRI, or a pharmaceutically acceptable salt or solvate thereof, and an amount of a GR antagonist, or a pharmaceutically acceptable salt or solvate thereof, optionally in association with one or more pharmaceutically acceptable carriers for use as therapy for depression and related disorders. | 10-16-2008 |
20080207598 | INDOLE DERIVATIVES - The invention relates to indole derivative having the general Formula I | 08-28-2008 |
20080207571 | Regimens for Oral Monophasic Contraceptives - The subject invention provides for new regimens for monophasic oral contraceptives. | 08-28-2008 |
20080200671 | Crystal form of asenapine maleate - The invention relates to an orthorhombic crystal form of compound trans-5-chloro-2,3,3a, 12b-tetrahydro-2-methyl-1H-dibenz [2,3:6,7] oxepino [4,5-c] pyrrole (Z)-2-butenedioate, to methods for the preparation of this crystal form and to pharmaceutical compositions comprising an orthorhombic crystal form. | 08-21-2008 |