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| Number | Title | Issue Date |
| 8183374 | Piperidine and piperazine derivatives Compounds of general formula (Ia): in which R1, A1, m, X, n, Y and R3 have any of the meanings given in the specification, have affinity for sigma receptors and are useful in the treatment of disor... | 05/22/2012 |
| 8093387 | Process of making crystalline type II aripiprazole Crystalline aripiprazole Type II can be formed without solid state heat treatment. Instead a liquid is used such as in crystallizing from a solvent, especially 2-propanol, dimethyl sulfoxide, or a combination thereof with ethyl acetate, or in a solvent mediated soli... | 01/10/2012 |
| 8039621 | Process for preparing anhydrous Aripirazole type I Type I anhydrous aripiprazole is prepared by dissolving aripiprazole (or an acid salt thereof) in an alcoholic solvent, optionally containing water, at elevated temperature, adding seed crystals of Type 1 anhydrous aripiprazole to the solution, cooling the mixture, ... | 10/18/2011 |
| 8008490 | Polymorphic forms of aripiprazole and method The present invention relates to novel polymorphic forms of aripiprazole and processes for producing them. It further relates to pharmaceutical compositions comprising the novel forms and to the use of the novel forms in the treatment of schizophrenia. ... | 08/30/2011 |
| 7943769 | Fluorinated derivative of quinolin-2(1H)-one, method for preparing the same and use thereof as a synthesis intermediate The invention relates to a fluorinated derivate of quinolin-2(1H)-one (I), to a method for preparing the same, and to the use thereof as an intermediate in the synthesis of 7-fluoro-2-oxo-4-[2-[4-[thieno[3,2-c]pyridine-4-yl)piperazin-1-yl]ethyl]-1,2-dihydro-quinolin... | 05/17/2011 |
| 7884205 | Salts of aripiprazole The present invention relates to acid addition salts of aripiprazole, a process for preparing said acid addition salts and their use to prepare or purify aripiprazole in the form of a free base or in the form of a pharmaceutically acceptable salt. ... | 02/08/2011 |
| 7872132 | Intermediates useful for the preparation of aripiprazole and methods for the preparation of the novel intermediates and aripiprazole An improved process for the preparation of aripiprazole (1) which comprises (i) reacting 6-hydroxy-l-indanone (11) with 1,4-dihalobutane (12) in the presence of a base and a solvent at a temperature in the range of 90 to 110 deg C to form the novel intermediate 6-(4... | 01/18/2011 |
| 7812162 | Enantiomers of 2′-fluoralkyl-6-nitroquipazine as serotonin transporter positron emission tomography imaging agents and antidepressant therapeutics Racemic mixtures and individual enantiomers of fluorine-18 or carbon-11 radio-labelled 2′-alkyl-6-nitroquipazine ligands are serotonin transporter (SERT) tracers for positron emission tomography (PET) imaging. The non-radioactive ligand forms possess therapeutic a... | 10/12/2010 |
| 7781585 | Crystalline forms of Gatifloxacin The present invention relates to a process for purification of novel polymorphic form of Gatifloxacin which comprises dissolving Gatifloxacin in about 15-50 volumes of methanol, removing insolubles if any, adding organic base to the solution, maintaining the solutio... | 08/24/2010 |
| 7714129 | Methods of preparing anhydrous aripiprazole form II Provided is a method of preparing aripiprazole anhydrous Form II from aripiprazole. ... | 05/11/2010 |
| 7655798 | Process of making crystalline Type II aripiprazole Crystalline aripiprazole Type II can be formed without solid state heat treatment. Instead a liquid is used such as in crystallizing from a solvent, especially 2-propanol, dimethyl sulfoxide, or a combination thereof with ethyl acetate, or in a solvent mediated soli... | 02/02/2010 |
| 7642353 | Process of making crystalline aripiprazole Crystalline aripiprazole Form B can be formed by crystallizing from a solvent selected from 1-propanol, 2-propanol, 1-butanol, ethyl acetate, acetonitrile or a combination thereof. ... | 01/05/2010 |
| 7601837 | Quinoline derivatives and their use as 5-HT6 ligands The present invention relates to novel quinoline compounds having pharmacological activity, to processes for their preparation, to compositions containing them and to their use in the treatment of CNS and other disorders. ... | 10/13/2009 |
| 7582762 | Salt and crystalline forms of (2R)-anti-5-{3-[4-(10,11-difluoromethanodibenzosuber-5-YL)piperazin-1-YL]-2-hydroxypropoxy}quinoline The present invention provides methods of treating leukemia comprising administration of a resistance modulating amount of a compound having the formula (2r)-anti-5-{3-[4-(10,11-difluoromethano-dibenzosuber-5-yl)piperazin-1-yl]-2-hydroxypropoxy}quinoline 2.5 hydroch... | 09/01/2009 |
| 7531656 | Synthesis of gatifloxacin Provided are a method for making (±)-1-Cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-(3-methyl-1-piperazinyl)-4-oxo-3-quinolenecarboxylic acid, commonly known as gatifloxacin, in high purity, in a suspension in a dipolar aprotic solvent. ... | 05/12/2009 |
| 7504504 | Methods of preparing aripiprazole crystalline forms The invention encompasses aripiprazole crystalline forms, methods of preparing the same, and pharmaceutical compositions having aripiprazole crystalline forms. ... | 03/17/2009 |
| 7491726 | Crystalline forms of aripiprazole The present invention provides novel crystalline forms of aripiprazole and aripiprazole hydrochloride, processes for their preparation and pharmaceutical compositions containing them. ... | 02/17/2009 |
| 7456181 | Aripiprazole crystalline forms The present invention provides novel crystalline forms of aripiprazole and processes for their preparation. ... | 11/25/2008 |
| 7442710 | Substituted phenyl methanones The present invention relates to compounds of general formula IA or IB wherein X1 and X2 are each independently N or C—R″ and R1, R2,R3, R... | 10/28/2008 |
| 7439244 | Quinoline compounds and pharmeceutical compositions containing them Disclosed are quinoline compounds of formula (I) having pharmacological activity, processes for their preparation, compositions containing them, and methods for the treatment of CNS and other disorders. ... | 10/21/2008 |
| 7439243 | Piperazinyl-quinoline derivatives useful for the treatment of CNS disorders Disclosed are quinoline compounds of formula (I) having pharmacological activity, processes for their preparation, compositions containing them, and methods for the treatment of CNS and other disorders. ... | 10/21/2008 |
| 7432264 | Antimicrobial biaryl compounds Provided are antibacterial biaryl compounds having micromolar MIC activity against Gram-negative and Gram-positive pathogens, including a methicillin-resistant S. aureus strain. ... | 10/07/2008 |
| 7432374 | Inhibitors of macrophage migration inhibitory factor and methods for identifying the same Inhibitors of MIF are provided which have utility in the treatment of a variety of disorders, including the treatment of pathological conditions associated with MIF activity. The inhibitors of MIF have the following structures: | 10/07/2008 |
| 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 |
| 7429585 | Phenyl-piperazine methanone derivatives, substituted by heterocyclic groups The present invention relates to compounds of the general formula IC wherein R2, R′, R″, R3, R6, X1 and X1′ are as defined here... | 09/30/2008 |
| 7423153 | Crystalline forms of gatifloxacin Provided are novel crystalline forms of gatifloxacin denominated forms A, B, C, D, E1, F, G, H, I, and J, and methods for their preparation. Also provided are methods for making known crystalline forms of gatifloxacin, in particular forms omega and T2RP. ... | 09/09/2008 |
| 7414047 | Piperazinyl and diazapanyl benzamides and benzthioamides Substituted piperazinyl and diazepanyl benzamides and benzthioamides of formula (I), compositions containing them, and methods of making and using them to treat histamine-mediated conditions. ... | 08/19/2008 |
| 7411067 | Crystalline forms of gatifloxacin Provided are two novel crystalline forms of gatifloxacin, denominated form O and form V, and methods for their preparation. ... | 08/12/2008 |
| 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 |
| 7402583 | Substituted quinolines as antitumor agents The invention provides a compound of Formula (Ia), or a pharmaceutically acceptable salt thereof, a process for t he preparation of a compound of Formula (1a) and pharmaceutical compositions of a compound of Formula ... | 07/22/2008 |
| 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 |
| 7388012 | (Hydrazido)(amino)thiophene compounds Compounds represented by Formula (I): or a pharmaceutically acceptable salt or N-oxide thereof, wherein A and J are defined herein, are useful in the treatment of tumors and cancers such as mastocytosis/mast cell leukemia, ... | 06/17/2008 |
| 7371765 | Quinoline derivatives having VEGF inhibiting activity The invention relates to compounds of formula (I) wherein: either any one of G1, G2, G3, G4 and G5 is nitrogen and the other four are —CH—, or G1, G2, G3, G4 and G... | 05/13/2008 |
| 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 |
| 7361756 | Method of making 7-(4-bromobutoxy)-3,4-dihydrocarbostyril The invention encompasses synthesizing 7-(4-bromobutoxy)-3,4-dihydrocarbostyril by mixing 7-hydroxy-tetrahydroquinolinone, dibromobutane, and at least one base to form a reaction mixture; heating the reaction mixture; cooling the reaction mixture; and isolating the ... | 04/22/2008 |
| 7351822 | Serine protease inhibitors Compounds of formula (I) in which R2, X, Y, Cy, L and Lp(D)n have the meanings given in the specification, are inhibitors of the serine protease, Factor Xa and are useful in the treatment of cardiovasc... | 04/01/2008 |
| 7332495 | Aralkyl-ketone piperazine derivatives and their uses as new antalgic or ataractic agent Arylalkyl ketone piperazine derivatives of the formula: and pharmaceutical compositions comprising the same. Also disclosed are methods for using the compounds as analgesic and sedative agents. The compounds of t... | 02/19/2008 |
| 7329749 | Piperazinylcarbonylquinolines and -isoquinolines Compound of the formula (I) in which R1, R2 and alk are as defined in Claim 1, are potent 5-HT2A antagonist and are suitable for the treatment of psychoses, schizophrenia, depression, neurological disorders, memory disorders, Parkins... | 02/12/2008 |
| 7326720 | Phenyl- and pyridylpiperidines with TNF activity The present invention relates to compounds of formula (I): in which X represents N or CH; R1 represents a hydrogen or halogen atom or a CF3 group; R2 and R3 independent... | 02/05/2008 |
| 7326710 | Aralkyl formyl-alkyl piperazine derivatives and their uses as a cerebral nerve protective agent Aralkyl formyl alkyl piperazine derivatives Pharmaceutical compositions comprising the same, and methods of using them as a neuroprotective agent. Pharmaceutical results indicate that these compounds have excelle... | 02/05/2008 |
