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| 20080300276 | Heterocyclic Carboxylic Acide Amide Derivatives - The invention relates to new heterocyclic carboxylic acid amide derivatives of formula (I)—wherein the meaning of X is hydrogen or halogen atom, hydroxy, cyano, C | 12-04-2008 |
| 20080312222 | 4-Benzyledene-Piperidin Derivatives - The present invention relates to new 4-benzylidene-piperidin derivatives of formula (I), useful as NMDA, in a particular NR2B subunit containing receptor antagonists and analgesica. | 12-18-2008 |
| 20090012118 | Kynurenic Acid Amide Derivatives as Nr2b Receptor Antagoni - The new kynurenic acid amide derivatives of formula (I): and optical antipodes, racemates and the salts thereof are highly effective and selective antagonists of NMDA receptor, and moreover most of the compounds are selective antagonist of NR2B subtype of NMDA receptor. | 01-08-2009 |
| 20090048303 | Indole-2-carboxamidine derivatives as nmda receptor antago - The present invention relates therefore first to new indole-2-carboxamidine derivatives of formula (I)—wherein the meaning of X is hydrogen or halogen atom, C | 02-19-2009 |
| 20090170901 | Benzoyl Urea Derivatives - The new benzoyl urea derivatives of formula (I) wherein the meaning of X and Y independently are hydrogen atom, hydroxy, benzyloxy, amino, nitro, C | 07-02-2009 |
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| 20090082818 | Canulated titanium implant for correcting flat feet in children - It is possible to satisfy all the requirements of minimal invasiveness with maximal permanent result by placing the invented implants (screw). The shape of the screw solves all mentioned technical problems that occurred thus far, i.e. it can be directed through a small gap in the skin by Kirschner's guide-wire (because the screw is hollow-canulated). The screw is larger in body, so a much greater force is needed for it to break. If it does break, it can be removed easier with less lesions to the surrounding bone tissue. At the point of the screw are trisect cuts (on the apex thread) which also make the lesion of the bone lesser as is as it is inserted in its position. Since the head of the screw is bigger and conical, without a narrow part leading to the screw-thread, the screw self-tightens into the bone, which makes the loosening rarer. The loosening is also rarer because of the shape of the screw-thread. The screw has the equal effect throughout the whole time it is implanted in the body. The osteolysis of the heel bone in which the screw stems against is also reduced. The conical shape of the head of the screw, without a narrow part (neck) between the head and the screw-thread, it does not allow ingrowing of the bone tissue, so it can be easily removed when the necessary time of correction is finished. The time necessary for the surgical procedure is significantly shorter, taking up 15 minutes, thus reducing the possibility of a infection, which is also helped by a small operative area. After the placement of the screw, the patient can walk two days after the surgery and he/she does not need any plaster immobilization or physical therapy. The screw is made out of titanium alloy, which gives it a certain toughness; the patient can undergo magnetic examinations, if there is need for such, while the screw is implanted. | 03-26-2009 |
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| 20080300240 | PDE10 INHIBITORS AND RELATED COMPOSITIONS AND METHODS - Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. The compounds have the general structure: | 12-04-2008 |
| 20110021509 | PDE10 INHIBITORS AND RELATED COMPOSITIONS AND METHODS - Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. The compounds have the general structure: | 01-27-2011 |
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| 20080306271 | Novel Process for Production of Highly Pure Polymorph (I) Donepezil Hydrochloride - The present invention provides a novel, industrially realizable and economically preferable process for production of highly pure 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methyl piperidine hydrochloride, i.e., donepezil hydrochloride shown in the following reaction scheme, in Polymorph (I) morphological crystal form. (I) In one of the key steps of the process, during the hydrogenation 5,6-dimethoxy 2-(pyridine-4-yhnethylene)indan- | 12-11-2008 |
| 20090093635 | PROCESS FOR MAKING POLYMORPH FROM I OF (S) - (+) -METHYL-ALPHA- (2-CHLOROPHENYL) -6, 7-DYHIDRO-THIENO- [3, 2-c] PYRIDINE-5 (4H) -ACETATE HYDROGEN SULFATE - The invention relates to a process for the preparation of the pharmaceutically applicable polymorph Form I of (S)-(+)-methyl-α-(2-chlorophenyl)-6,7-dyhidro-thieno[3,2-c]-pyridine-5(4H)-acetate hydrogen sulfate of formula I; by reacting (S)-(+)-methyl-α-(2-chlorophenyl)-6,7-dyhidro-thieno[3,2-c]pyridine-5(4H)-acetate and sulfuric acid in the presence of solvents which comprises dissolving (S)-(+)-methyl-α-(2-chlorophenyl)-6,7-dyhidro-thieno[3,2-c]pyridine-5(4H)-acetate in an ether; mixing this solution with a solution of a C | 04-09-2009 |
| 20090111988 | NOVEL PROCESS FOR PRODUCTION OF 5--6-CHLORO-1,3-DIHYDRO-2H-INDOL-2-ONE (ZIPRASIDONE) - The present invention provides a novel, industrially easily realisable and economically preferable process for production of pure 5-{2-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]-ethyl}-6-chloro-1,3-dihydro-2H-indol-2-one i.e., ziprasidone hydrochloride shown in the reaction scheme (II), (III), (IV), (V) and (VI). According to the invention the intermediate compound 5-(2-bromoethyl)-6-chloro-1,3-dihydro-2H-indol-2-one of Formula (III) is produced from 5-(2-bromoacethyl)-6-chloro-1,3-dihydro-2H-indole-2-one of Formula (IV). The highly pure ziprasidone base of Formula (II) is obtained in the reaction of 3-piperazinyl-1,2-benzisothiazol of Formula (VI) with 5-(2-bromoethyl)-6-chloro-1,3-dihydro-2H-indol-2-one of Formula (III) in an organic solvent or organic solvent mixture. | 04-30-2009 |
| 20100081668 | POLYMORPHS OF 5--6-CHLORO-1,3-DIHYDRO-2H-INDOL-2-ONE HYDROBROMIDE AND PROCESSES FOR PREPARATION THEREOF - The present invention provides pharmaceutically applicable compounds and polymorphs belonging to the ziprasidone hydrobromide compound group with antipsychotic effect. The present invention provides hydrobromide polymorphs of 5-{-2-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]-ethyl}-6-chloro-1,3-dihydro-2H-indol-2-one, ziprasidone of Formula (I) having neuroleptic activity. | 04-01-2010 |
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| 20080200668 | Industrial Process for the Preparation of 17-Hydroxy-6Beta, 7Beta; 15Beta, 16Beta-Bismethylene-3-Oxo-17Alpha-Pregn-4-Ene-21-Carboxylic Acid Y-Lactone and Key Intermediates for this Process - The invention relates to an industrial process for the preparation of 17-hydroxy-6β,7β;15β,16β-bismethylene-3-oxo-17α-pregn-4-ene-21-carboxylic acid γ-lactone of formula (I), and to the key-intermediates for this process. | 08-21-2008 |
| 20080287404 | High Purity 17Alpha-Cyanomethyl-17Beta-Hydroxy-Estra-4,9-Diene-3- One and Process For the Syntheses Thereof - The invention relates to a new process for the synthesis of high purity 17α-cyanomethyl-17β-hydroxy-estra-4,9-diene-3-one (further on dienogest) of formula (I) from 3-methoxy-17-hydroxy-estra-2,5(10)-diene of formula (V). The invention relates also to the high purity 17α-cyanomethyl-17β-hydroxy-estra-4,9-diene-3-one and pharmaceutical compositions containing that as active ingredient. The pharmaceutical compositions according to this invention contain high purity dienogest of formula (I) in which the total amount of impurities is less than 0.1%, while the amount of 4-bromo-dienogest is under the detection limit (0.02%) as active ingredient or at least one of the active ingredients and auxiliary materials, which are commonly used in practice, such as carriers, excipients or diluents. According to our invention the dienogest of formula (I) is synthesized the following way: i) 3-methoxy-17-hydroxy-estra-2,5(10)-diene of formula (V) is reacted with aluminum isopropylate in the presence of cyclohexanone in an inert organic solvent under heating; ii) the so obtained 3-methoxy-estra-2,5(10)-diene-17-one of formula (IV) is reacted with cyanomethyl lithium at a temperature between 0 and −30° C.; iii) the obtained 3-methoxy-17α-cyanomethyl-17β-hydroxy-estra-2,5(10)-diene of formula (III) is reacted with a strong organic acid in tetrahydrofuran solution; iv) the obtained 17α-cyanomethyl-17β-hydroxy-estr-5(10)-ene-3-one of formula (II) is reacted with 1-1.5 equivalent of pyridinium tribromide in pyridine solution at a temperature between 0 and 60° C., then the obtained crude dienogest of formula (I) is purified by recrystallization and preparative HPLC. | 11-20-2008 |
| 20090312299 | Isolated Isomers of Norelgestromin and Methods of Making and Using the Same - The invention is directed to a process of preparing substantially pure d-(17α)-13-ethyl-17-hydroxy-18,19-dinorpregn-4-ene-20-yn-3-one-3E- and -3Z-oxime isomers, as well as a process for the synthesis of the mixture of isomers and the pure isomers. The invention also relates to substantially pure d-(17α)-13-ethyl-17-hydroxy-18,19-dinorpregn-4-ene20-yn-3-one-3E-oxime and substantially pure d-(17α)-13-ethyl-17-hydroxy-18,19-dinorpregn-4-ene-20-yn-3-one-3Z-oxime isomer. Further aspects of the invention include a composition comprising substantially pure d-(17α)-13-ethyl-17-hydroxy-18,19-dinorpregn-4-ene20-yn-3-one-3E-oxime or substantially pure d-(17α)-13-ethyl-17-hydroxy-18,19-dinorpregn-4-ene-20-yn-3-one-3Z-oxime isomer, and methods of treatment using said compositions. | 12-17-2009 |
| 20100137622 | INDUSTRIAL METHOD FOR THE SYNTHESIS OF 17-ACETOXY-11beta-[4-(DIMETHYLAMINO)-PHENYL]-21-METHOXY-19-NORPREGNA-4,9-- DIEN-3,20-DIONE AND THE KEY INTERMEDIATES OF THE PROCESS - The present invention relates to a process for the synthesis of the known 17-acetoxy-11-β-[4-(dimethyl amino)-phenyl]-21-methoxy-19-norpregna-4,9-dien-3,20-dione (further on CDB-4124) of formula (I) from 3,3-[1,2-ethandiyl-bis(oxy)]-oestr-5(10),9(11)-dien-17-one of formula (II). Compound CDB-4124 belongs to the group of anti-hormones. The process has the following steps: i) formation of an epoxide; ii) addition of hydrogen cyanide; iii) silylation of a hydroxyl group; iv) reaction with 4-(dimethylamino)-phenyl magnesium bromide Grignard reagent in the presence of CuCl (Teutsch reaction); v) silylation of a hydroxyl group with trimethyl chlorosilane; vi) reaction with diisobutyl aluminum hydride and after addition of acid to the reaction mixture; vii) methoxy-methylation with methoxy-methyl Grignard reagent formed in situ, while hydrolyzing the trimethylsilyl protective groups; viii) oxidation of a hydroxyl group with dicyclohexyl carbodiimide in the presence of dimethyl sulfoxide and a strong organic acid (Swern oxidation), and in given case after purification by chromatography; ix) acetylation of a hydroxyl group with acetic anhydride in the presence of perchloric acid, and in given case, purification by chromatography. The invention also relates to new intermediates of the process. | 06-03-2010 |
