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| Number | Title | Issue Date |
| 8143258 | Benzothiazole compounds useful for Raf inhibition Provided is a fused heterocycle derivative showing a strong Raf inhibitory activity. A compound represented by the formula wherein each symbol is as defined in the present specification, or a salt thereof. ... | 03/27/2012 |
| 8106056 | Combination preparations comprising bifeprunox and a dopamine agonist The present invention relates to a composition containing bifeprunox or its N-oxide, or at least one pharmacologically acceptable salt thereof: and L-DOPA or at least one pharmacologically acceptable salt thereof, for simul... | 01/31/2012 |
| 8101619 | Phenylpiperazine derivatives with a combination of partial dopamine-Dreceptor agonism and serotonin reuptake inhibition The invention relates to a group of novel phenylpiperazine derivatives with a dual mode of action: serotonin reuptake inhibition and partial agonism on dopamine-D2 receptors. The invention also relates to the use of a compound disclosed herein for the man... | 01/24/2012 |
| 8088777 | Urea derivative Disclosed is a novel compound having an NPY Y5 receptor antagonistic activity. A compound represented by the formula: its pharmaceutically acceptable salt or solvate thereof, wherein X is hydrogen... | 01/03/2012 |
| 7964604 | Bifeprunox mesylate maintenance dose compositions and methods for using the same The present disclosure provides novel pharmaceutical dosage forms such as a maintenance treatment dose and methods for making the same, and methods for using said compounds and maintenance treatment doses to treat and prevent diseases and/or disorders. ... | 06/21/2011 |
| 7943623 | Pharmaceutical composition comprising 2,3-dihydro-6-nitroimidazo [2,1-B] oxazole derivatives A pharmaceutical composition according to the present invention comprises: (I) at least one member selected from the group consisting of oxazole compounds, optically active isomers thereof, and salts thereof, the oxazole compounds being represented by general formul... | 05/17/2011 |
| 7915262 | Combination preparations comprising SLV308 and a dopamine agonist A composition containing SLV308 or its N-oxide, or at least one pharmacologically acceptable salt thereof: and L-DOPA or at least one pharmacologically acceptable salt thereof, for simultaneous, separate or sequential use i... | 03/29/2011 |
| 7893067 | Cysteine protease inhibitors Compounds of the formula II: wherein R2 is the side chain of leucine, isoleucine, cyclohexylglycine, O-methyl threonine, 4-fluoroleucine or 3-methoxyvaline; R3 is H, methyl or F; | 02/22/2011 |
| 7799791 | Tetrahydrofuro(3,2-B) pyrrol-3-one derivatives as inhibitors of cysteine proteinases A compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof, wherein: one of R1 and R2 is H, and the other is selected from OR6, SR6, NR... | 09/21/2010 |
| 7790726 | Monocyclic and bicyclic compounds and methods of use Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally monocyclic and bicyclic compounds and are useful in pharmaceutical compositions, methods for the treatment of CCR1-me... | 09/07/2010 |
| 7786126 | Combination preparations comprising SLV308 and a dopamine agonist A composition containing SLV308 or its N-oxide, or at least one pharmacologically acceptable salt thereof: and L-DOPA or at least one pharmacologically acceptable salt thereof, for simultaneous, separate or sequential use i... | 08/31/2010 |
| 7767682 | Medicaments Methods of prevention or treatment of renal diseases or conditions associated with abnormal ion flux, in particular autosomal dominant polycystic kidney disease, with a modulator of human peroxisome proliferator activated receptor gamma. ... | 08/03/2010 |
| 7767681 | 2-Carbamide-4-phenylthiazole derivatives, preparation thereof and therapeutic use thereof The disclosure concerns 2-carbamide-4-phenylthiazole derivatives of general formula (I). The disclosure also concerns pharmaceutical compositions containing a compound of general formula (I) and to processes for preparing and methods of using compounds of general fo... | 08/03/2010 |
| 7750013 | N-oxides as prodrugs of piperazine and piperidine derivatives The present disclosure relates to N-oxides of certain piperazine and piperidine derivatives and to methods for the preparation of these compounds. The disclosure also relates to the use of the compounds for the manufacture of a medicament giving a beneficial effect.... | 07/06/2010 |
| 7718659 | Heteroarylacetamide inhibitors of factor Xa The invention is concerned with novel heteroarylacetamides of formula (I) Rd—C(O)—N(Re)—Rc—CH2—C(O)—N(Ra)(Rb) (I) wherein Ra to Re are as def... | 05/18/2010 |
| 7713979 | Cycloalkyl lactam derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1 The present invention discloses compounds of Formula I: (I) having 11beta-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, a... | 05/11/2010 |
| 7605162 | Phenylpiperazine The invention relates to a novel group of phenylpiperazines having interesting pharmacological properties such as a high affinity for the dopamine D2 receptor and/or the serotonin reuptake site, and the ability to treat conditions related to disturbances ... | 10/20/2009 |
| 7544687 | Substituted α-piperazinyl phenylpropionic acid derivatives as hPPAR α and/or hPPAR γ agonists The present invention relates to a compound of formula I, racemates, optically active isomers, or pharmaceutically acceptable salts or solvates thereof, and a pharmaceutical composition comprising the compound, the various radicals in the formula I are the same as d... | 06/09/2009 |
| 7531542 | Benzooxazole and benzothiazole antagonists of gonadotropin releasing hormone receptor The present invention relates to Gonadotropin Releasing Hormone (GnRH, also known as Luteinizing Hormone Releasing Hormone) receptor antagonists. ... | 05/12/2009 |
| 7514439 | Oxime derivative and preparations thereof The problem of the present invention is to provide a useful compound as a glucokinase activating agent, which is the oxime derivative of the formula [I]: wherein Ring A is aryl or heteroaryl; ... | 04/07/2009 |
| 7501421 | Benzoxazole and benzothiazole derivatives as 5-hydroxytryptamine-6 ligands The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor. ... | 03/10/2009 |
| 7494998 | Benzisoxazole piperazine compounds and methods of use thereof The invention includes benzisoxazole piperazine compositions and methods of using them for modulating sleep. ... | 02/24/2009 |
| 7456182 | Phenylpiperazines The invention relates to a novel group of phenylpiperazines having interesting pharmacological properties such as a high affinity for the dopamine D2 receptor and/or the serotonin reuptake site, and the ability to treat conditions related to disturbances ... | 11/25/2008 |
| 7452889 | Substituted heterocyclic compounds Disclosed are novel substituted heterocyclic derivatives having the structure of Formula I: The compounds are useful for the treatment of various disease states, in particular cardiovascular diseases such as atrial and vent... | 11/18/2008 |
| 7449468 | Thiazole and oxazole derivatives as activators of human peroxisome proliferator activated receptors The present invention provides a compound of formula (I): wherein R1-R5, R25, R26, Y, y, and X2are as defined herein. The compounds activate hu... | 11/11/2008 |
| 7435738 | Stable crystalline form of bifeprunox mesylate (7-[4-([1,1′-biphenyl]-3-ylmethyl)-1-piperazinyl]-2(3H)-benzoxazolone monomethanesulfonate) The invention relates to a stable polymorphic form of the compound 7-[4-([1,1′-biphenyl]-3-ylmethyl)-1-piperazinyl]-2 (3H)-benzoxazolone monomethanesulfonate (INNM bifeprunox mesylate), a method for the preparation of said polymorphic form and its use in pharmaceu... | 10/14/2008 |
| 7432269 | Arylpiperaszine derivatives, to the process for the production thereof and to the use thereof as therapeutic agents The invention relates to compounds of the general formula (I): to the process for preparing them, and to the use thereof as a therapeutic agent having the property of being selective ligands for the dopamine D3 receptor. Th... | 10/07/2008 |
| 7423040 | Stable crystalline form of bifeprunox mesylate, dosage forms thereof and methods for using same The present disclosure provides novel pharmaceutical compounds and methods for making the same, novel pharmaceutical dosage forms and methods for making the same, and methods for using said compounds and dosage forms to treat and prevent diseases and/or disorders. | 09/09/2008 |
| 7407960 | Substituted heterocyclic compounds Disclosed are novel heterocyclic compounds having the structure which are useful for the treatment of various disease states, in particular cardiovascular diseases such as atrial and ventricular arrhythmias, intermittent cl... | 08/05/2008 |
| 7405216 | Stable crystalline form of bifeprunox mesylate (7-[4-([1,1′-biphenyl]-3-ylmethyl)-1-piperazinyl]-2(3H)-benzoxazolone monomethanesulfonate) The invention relates to a stable polymorphic form of the compound 7-[4-([1,1′-biphenyl]-3-ylmethyl)-1-piperazinyl]-2(3H)-benzoxazolone monomethanesulfonate (INNM bifeprunox mesylate), a method for the preparation of said polymorphic form and its use in pharmaceut... | 07/29/2008 |
| 7405217 | N-aroyl piperazine derivatives as orexin receptor antagonists This invention relates to N-aroyl cyclic amino derivatives and their use as pharmaceuticals. ... | 07/29/2008 |
| 7396830 | Piperazine amidines as antiviral agents This disclosure provides compounds of Formula I as described herein having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the disclosure is concerned with indole and a... | 07/08/2008 |
| 7396834 | 4(Phenyl-piperazinyl-methyl) benzamide derivatives and their use for the treatment of pain or gastrointestinal disorders Compounds of general formula: wherein R1 and R2 are as defined in the specification, as well as salts, enantiomers thereof and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the ma... | 07/08/2008 |
| 7365077 | Piperazine bis-amide derivatives and their use as antagonists of the orexin receptor Disclosed are piperazine bis-amide derivatives useful as antagonists of the orexin receptor and pharmaceutical compositions containing the same. ... | 04/29/2008 |
| 7361654 | Substituted heteroaryl amide modulators of glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof The present invention relates to new class of non-steroidal compounds which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity including obesity, diabetes, inflammatory- and immune-associated disea... | 04/22/2008 |
| 7345043 | Inhibitors of histone deacetylase Disclosed are compounds which inhibit histone deacetylase (HDAC) enzymatic activity. Also disclosed are pharmaceutical compositions comprising such compounds as well as methods to treat conditions, particularly proliferative conditions, mediated at least in part by ... | 03/18/2008 |
| 7335660 | Isochroman compounds for treatment of CNS disorders This invention relates to compounds of formula (I) where R1 to R12, —W—V—, —X—Y—, p and n have the values defined in claim 1, their preparation and use as pharmaceuticals for the tre... | 02/26/2008 |
| 7319097 | Compounds The present invention relates to substituted bis-arylsulfonamide and arylsulfonamide compounds of the general formula (I) or the formula (II), which compounds are potentially useful for the prophylaxis and treatment of medical conditions relating to obesity, type II... | 01/15/2008 |
| 7309715 | Compound A compound having Formula I wherein one of R1 and R2 is a group of the formula wherein R4 is selected from H and hydrocarbyl... | 12/18/2007 |
| 7300939 | Substituted 1-propiolylpiperazine compounds, their preparation and use Substituted 1-propiolylpiperazine compounds corresponding to formula I in which X denotes N or C—R2, and n is an integer from 0 to 8, a method for producing such substituted 1-propiolylpiperazine com... | 11/27/2007 |
