Nitrogen Attached Directly Or Indirectly To The Hetero Ring By Acyclic Nonionic Bonding Patents (Class 549/467)
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Publication number: 20090093485Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof; compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating the glucocorticoid receptor in a warm blooded animal).Type: ApplicationFiled: October 26, 2005Publication date: April 9, 2009Applicant: ASTRAZENECA ABInventors: Hakan Bladh, Krister Henriksson, Vijaykumar Hulikal, Matti Lepisto
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Publication number: 20090088469Abstract: Method for the preparation of citalopram comprising reaction of a compound of Formula (IV) wherein R is halogen, or CF3—(CF2)n—SO2—, n being 0 to 8, with a cyanide source in the presence of a palladium catalyst and a catalytic amount of Cu+ or Zn2+, or with Zn(CN)2 in the presence of a palladium catalyst.Type: ApplicationFiled: December 8, 2008Publication date: April 2, 2009Applicant: H. Lundbeck A/SInventors: Hans Petersen, Michael Harold Rock, Henrik Svane
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Patent number: 7511161Abstract: A process of purifying citalopram, either in racemic or enantiomeric form, which process comprises (i) providing a crude mixture comprising citalopram, either in racemic or enantiomeric form, dissolved in a water immiscible organic solvent, and which mixture also includes one or more citalopram derivatives which are present as citalopram impurities; (ii) washing the crude mixture with at least one dilute aqueous solution of a polybasic acid, either in free form or as a partial alkali metal salt, so as to separate citalopram from citalopram impurities present in the crude mixture; and (iii) where required converting citalopram free base, separated from citalopram impurities further to step (ii), to a pharmaceutically acceptable salt.Type: GrantFiled: July 23, 2004Date of Patent: March 31, 2009Assignee: Meditab Specialities Pvt. Ltd.Inventors: Sunil Govindrao Uttarwar, Bhagwan Narayan Gawli
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Publication number: 20090082582Abstract: The invention relates to a process for the preparation of compounds of general formula (3) wherein: (a) represents a single or double bond; W represents a group CH, CH2, CHCH3, CCH3, C(CH3)2, a group C(CH2)2 (i.e. a carbon atom carrying two methylene groups bonded to one another so as to form a spiro-cyclopropane moiety), with the proviso, however, that when (a) is a double bond then W represents exclusively a group CH or CCH3 and when (a) is a single bond then W represents exclusively a group CH2, CHCH3, C(CH3)2 or C(CH2)2.Type: ApplicationFiled: March 8, 2007Publication date: March 26, 2009Applicant: Pierre Fabre MedicamentInventors: Bernard Vacher, Stephane Cuisiat, Nicolas Roques
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Publication number: 20090076137Abstract: The present application describes deuterium-enriched dronedarone, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: August 21, 2008Publication date: March 19, 2009Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
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Publication number: 20090075938Abstract: There are disclosed compound of Formula (1): A1, A2, A3 and A4 which may be the same or different, represent N or CR1, X is a divalent group selected from O, S(O)n, C?W, NR4, NC(?O)R5 and CR6R7, W is O, S, NR20, Y is N or CR8, one of R4, R5, R6, R8, R9 and NR20 represents -L-R3, in which L is a single bond or a linker group, additionally, R1, R3-R9, which may be the same or different, independently represent hydrogen or a substituent and R20 represents hydrogen, hydroxyl, alkyl optionally substituted by aryl, alkoxy optionally substituted by aryl, aryl, CN, optionally substituted alkoxy, optionally substituted aryloxy, optionally substitute alkanoyl, optionally substituted aroyl, NO2, NR30R31, in which R30 and R31, which may be the same or different, represent hydrogen, optionally substituted alkyl or optionally substituted aryl; additionally, one of R30 and R31 may represent optionally substituted alkanoyl or optionally substituted aroyl, n represents an integer from 0 to 2, in addition, when an adjacent paiType: ApplicationFiled: February 9, 2007Publication date: March 19, 2009Inventors: Graham Michael Wynne, Stephen Paul Wren, Peter David Johnson, Paul Damien Price, Olivier De Moor, Gary Nugent, Richard Storer, Richard Joseph Pye, Colin Richard Dorgan
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Publication number: 20090069582Abstract: This patent discloses a method for resolution of 4-[4-(dimethylamino)-1-(4?-fluorophenyl)-1-hydroxybutyl]-3-(hydroxymethyl)-benzonitrile as a racemic or non-racemic enantiomer mixture into its isolated enantiomers, said method comprising the step of fractionally crystallizing 4-[4-(dimethylamino)-1-(4?-fluoro-phenyl)-1-hydroxybutyl]-3-(hydroxymethyl)-benzonitrile as a salt with the (+)—(S,S)— or (?)—(R,R)-enantiomer of O,O?-di-p-toluoyl-tartaric acid in a solvent system comprising 1-propanol, ethanol or acetonitrile.Type: ApplicationFiled: September 2, 2008Publication date: March 12, 2009Applicant: H. Lundbeck A/SInventors: Carla De Faveri, Florian Anton Martin Huber, Robert Dancer
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Publication number: 20090054235Abstract: The present invention relates to novel benzoheterocyclylethylbenzamide derivatives of formula (I) in which the substituents are in the description, their process of preparation, their use as fungicides, particularly in the form of fungicidal compositions, and methods for the control of phytopathogenic fungi of plants using these compounds or their compositions.Type: ApplicationFiled: July 6, 2006Publication date: February 26, 2009Inventors: Darren Mansfield, Pierre-Yves Coqueron, Heiko Rieck, Philippe Desbordes, Alain Villier, Marie-Claire Grosjean-Cournoyer, Pierre Genix
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Publication number: 20090048336Abstract: Escitalopram oxalate powders having definite particle size distribution parameters, processes for preparing the powders, and solid pharmaceutical formulations containing the powders.Type: ApplicationFiled: August 18, 2008Publication date: February 19, 2009Inventors: Naveen Kumar Kolla, Ravi Ram Elati, Srinivas Gangula
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Publication number: 20090042875Abstract: The present invention relates to substituted heterocyclic compounds and compositions comprising a substituted heterocyclic compound. The present invention also relates to methods for preventing or treating various diseases and disorders by administering to a subject in need thereof one or more substituted heterocyclic compounds. In particular, the invention relates to methods for preventing or treating cancer or an inflammatory disorder by administering to a subject in need thereof one or more substituted heterocyclic compounds. The present invention further relates to articles of manufacture and kits comprising one or more substituted heterocyclic compounds.Type: ApplicationFiled: September 29, 2008Publication date: February 12, 2009Inventors: George W. Muller, Hon-Wah Man
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Patent number: 7482476Abstract: A new process is described for obtaining 5-cyanophthalide, which is an intermediate used for the synthesis of citalopram and its active enantiomer S(+) citalopram, both of which are known active ingredients commonly used for treating depression. The process involves starting from 5-carboxyphthalide which is converted into the corresponding acylochloride. The latter is reacted with hydroxylamine to produce the corresponding hydroxamyl phthalide, which is subsequently subjected to a dehydration reaction to produce 5-cyanophthalide.Type: GrantFiled: October 13, 2006Date of Patent: January 27, 2009Assignee: Adorkem Technology SpAInventors: Giovanni Cotticelli, Raul Salvetti, Marco Zappa
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Patent number: 7482477Abstract: A process is described for the preparation of citalopram (I) and of the active enantiomer thereof, escitalopram (II), which process comprises the cyclisation reaction of the corresponding precursor diol of the formula III or, respectively, IV in the presence of an azodicarboxylate, a phosphine and a strong base.Type: GrantFiled: September 14, 2005Date of Patent: January 27, 2009Assignee: Adorkem Technology SPAInventors: Giovanni Cotticelli, Raul Salvetti
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Publication number: 20090023798Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of histone deacetylase. Also described herein are methods of using such HDAC inhibitors, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of HDAC activity.Type: ApplicationFiled: June 16, 2008Publication date: January 22, 2009Applicant: PHARMACYCLICS, INC.Inventors: Darren Magda, Zhong Wang
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Publication number: 20090018351Abstract: The present invention relates to a process for preparing enantiomerically enriched citalopram via methylating enantiomerically enriched didesmethylcitalopram, which is prepared by directly resolving racemic didesmethylcitalopram using a chiral acid.Type: ApplicationFiled: November 12, 2004Publication date: January 15, 2009Applicants: DR. REDDY'S LABORATORIES, INC., DR. REDDY'S LABORATORIES LTD.Inventors: Venkataraman Sundaram, Vijayavithai Thippannachar Mathad, Pravinachandra Jayanthilal Venkavala, Chandrashekar Ravirama Elati, Naveenkumar Kolla, Shanmugam Govindan, Subrahmanyeshwara Rao Chalamala, Srinivas Gangula
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Patent number: 7470526Abstract: A process for preparing an intermediate for synthesizing escitalopram and the pharmaceutically acceptable salts thereof from 4-(4-dimethylamino)-1-(4?-fluorophenyl)-1-(hydroxybutyl)-3-(acyloxymethyl)benzonitrile is described. The process involves converting said intermediate into the (S+) enantiomer of citalopram by means of enzymatic enantiomeric resolution.Type: GrantFiled: October 6, 2006Date of Patent: December 30, 2008Assignee: Adorken Technology SpAInventors: Giovanni Cotticelli, Silvia Rocchietti, Marco Terreni, Massimo Pregnolato, Raul Salvetti
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Patent number: 7470799Abstract: Compounds of formula I are provided: wherein each of R1, R2, y, m, n, and Ar are as defined, and described in classes and subclasses herein, which are agonists or partial agonists of melatoninergic receptors. The compounds, and compositions containing the compounds, can be used to treat melatoninergic disorders.Type: GrantFiled: April 21, 2006Date of Patent: December 30, 2008Assignee: WyethInventors: Gary Paul Stack, Jonathan Laird Gross
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Publication number: 20080318779Abstract: Conventional many fungicidal compositions have had practical problems such that either a preventive effect or a curing effect is inadequate, the residual effect tends to be inadequate, or the controlling effect against plant diseases tends to be inadequate depending upon the application site, and a fungicidal composition to overcome such problems has been desired.Type: ApplicationFiled: August 10, 2005Publication date: December 25, 2008Applicant: ISHIHARA SANGYO KAISHA LTDInventors: Yuji Nakamura, Shigeru Mitani, Tetsuo Yoneda
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Publication number: 20080312318Abstract: The present application describes deuterium-enriched escitalopram, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: June 14, 2007Publication date: December 18, 2008Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
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Publication number: 20080305164Abstract: Crystalline particles of escitalopram oxalate with a particle size of at least 40 ?m is disclosed. Method for the manufacture of said crystalline particles and pharmaceutical compositions comprising said crystalline particles are also disclosed.Type: ApplicationFiled: August 22, 2008Publication date: December 11, 2008Applicant: H. LUNDBECK A/SInventors: Troels Volsgaard Christensen, Ken Liljegren, Michiel Onne Elema, Lene Andresen, Shashank Mahashabde, Sebastian P. Assenza
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Publication number: 20080306041Abstract: The invention describes compositions and kits comprising at least one cardiovascular compound comprising at least one heterocyclic nitric oxide donor group, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating cardiovascular diseases; (b) treating renovascular diseases; (c) treating diabetes; (d) treating diseases resulting from oxidative stress; (e) treating endothelial dysfunctions; (f) treating diseases caused by endothelial dysfunctions; (g) treating cirrhosis; (h) treating pre-eclampsia; (j) treating osteoporosis; (k) treating nephropathy; (l) treating peripheral vascular diseases; (m) treating portal hypertension and (n) treating ophthalmic disorders. The cardiovascular compounds are preferably ?-adrenergic antagonists, angiotensin-converting enzyme (ACE) inhibitors, anti-hyperlipidemic compounds, and antithrombotic and vasodilator compounds.Type: ApplicationFiled: January 23, 2006Publication date: December 11, 2008Inventor: David S. Garvey
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Patent number: 7456162Abstract: Compounds represented by the formula: wherein R1 and R2 are hydrogen atom, a hydrocarbon group or a heterocyclic group, or R1 and R2 may form, together with the adjacent carbon atom, a 3- to 8-membered homocyclic or heterocyclic ring, W indicates a group represented by the formula: wherein R4 indicates (1) an aliphatic hydrocarbon group, which may be substituted with an aromatic group, or (2) an acyl group containing an aromatic group, R5 is hydrogen atom, a C1-6 alkyl, or an acyl group, R3 indicates a C6-14 aryl group, or salts thereof. The compounds have an excellent action to inhibit neurodegeneration as well as an excellent brain penetrability and are low in the toxicity, thereby being useful as drugs for nerve degenerative diseases.Type: GrantFiled: March 17, 2005Date of Patent: November 25, 2008Assignee: Takeda Pharmaceutical Company LimitedInventors: Shigenori Ohkawa, Yasuyoshi Arikawa, Kouki Kato, Masahiro Okura, Masaki Setoh
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Publication number: 20080287489Abstract: This invention relates to potent potassium channel blocker compounds of Formula I or a formulation thereof for the treatment of glaucoma and other conditions which leads to elevated intraocular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans.Type: ApplicationFiled: July 23, 2008Publication date: November 20, 2008Inventors: Dong-Ming Shen, James B. Doherty
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Publication number: 20080281110Abstract: The (S)-citalopram content of a mixture of (R)- and (S)-citalopram can be enriched by using L-tartaric acid as the resolving agent in the presence of formaldehyde.Type: ApplicationFiled: April 22, 2008Publication date: November 13, 2008Inventor: Jie Zhu
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Publication number: 20080262224Abstract: This invention relates to a method of preparation of benzofuran-2-carboxylic acid {(S)-3-methyl-1-[(4S,7R)-7-methyl-3-oxo-1-(pyridine-2-sulfonyl)-azepan-4-ylcarbamoyl]-butyl}-amide.Type: ApplicationFiled: January 21, 2005Publication date: October 23, 2008Inventors: William M. Clark, Neil Francis Badham, Qunying Dai, Ann Marie Eldridge, Hayao Matsuhashi
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Patent number: 7439368Abstract: The present invention provides a process of preparing a compound of the formula [I]: wherein X is a group of the formula: —N? or —CH?; R1 is a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a cyano group or an amino group optionally substituted by a lower alkyl group; Ring A is a nitrogen-containing heterocyclic group; Ring B is an optionally substituted benzene ring or an optionally substituted pyridine ring; and R3 is a hydrogen atom or a lower alkyl group, or a pharmaceutically acceptable salt thereof, which is useful as an inhibitor of activated blood coagulation factor X.Type: GrantFiled: June 29, 2004Date of Patent: October 21, 2008Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Masahiko Seki, Shin-ichi Yoshida, Nobuhiro Yagi, Masanori Hatsuda, Mayumi Kimura, Kazuhiko Kondo
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Publication number: 20080255230Abstract: Disclosed herein is compound having a formula as described herein. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: ApplicationFiled: March 28, 2008Publication date: October 16, 2008Inventors: Ken Chow, Wenkui K. Fang, Evelyn G. Corpuz, Daniel W. Gil, Michael E. Garst
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Patent number: 7435837Abstract: Compounds of Formula 1 or pharmaceutically acceptable salts thereof are provided: which are agonists or partial agonists of the 2C subtype of brain serotonin receptors. The compounds, and compositions containing the compounds, can be used to treat a variety of central nervous system disorders such as schizophrenia.Type: GrantFiled: October 21, 2004Date of Patent: October 14, 2008Assignee: WyethInventors: Jonathan Laird Gross, Marla Jean Williams, Gary Paul Stack, Hong Gao, Dahui Zhou
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Publication number: 20080221191Abstract: A method of treating a Mycobacterium tuberculosis infection in a subject in need thereof by administering to the subject an effective amount of a cationic substituted benzofuran compound. Methods of treating microbial infections, including infections from protozoan pathogens, such as Leishmania donovani, Trypanosoma brucei rhodesiense, a Trypanosoma cruzi, and Plasmodium falciparum, and fungal pathogens, such as Candida albicans, Aspergillus fumigatus, and Cryptococcus neoformans, in a subject in need thereof by administering to the subject an effective amount of a cationic substituted benzofuran compound. Methods of synthesizing novel cationic substituted benzofuran compounds and the novel compounds themselves.Type: ApplicationFiled: October 31, 2007Publication date: September 11, 2008Inventors: Richard R. Tidwell, Karl Werbovetz, Scott Gary Franzblau, Svetlana Bakunova, Stanislav Bakunov
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Patent number: 7420069Abstract: Crystalline particles of escitalopram oxalate with a particle size of at least 40 ?m is disclosed. Method for the manufacture of said crystalline particles and pharmaceutical compositions comprising said crystalline particles are also disclosed.Type: GrantFiled: February 7, 2005Date of Patent: September 2, 2008Assignee: H. Lundbeck A/SInventors: Troels Volsgaard Christensen, Ken Liljegren, Michiel Onne Elema, Lene Andresen, Shashank Mahashabde, Sebastian P. Assenza
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Patent number: 7420070Abstract: A process for preparing optically active 2,3-dihydrobenzofuran compounds which comprises subjecting a 2,3-dihydrobenzofuran compound represented by the general formula or a salt thereof to optical resolution with an optically active acid compound: [wherein R1 and R2 are each hydrogen or an optionally substituted hydrocarbon group; R3 is an optionally substituted aromatic group; and C is a benzene ring which may further have a substituent in addition to the amino group]. The process enables industrially advantageous production of intermediates for the synthesis of optically active 2,3-dihydrobenzofuran compounds useful as preventive and/or therapeutic drugs for neurodegenerative diseases and so on.Type: GrantFiled: February 9, 2005Date of Patent: September 2, 2008Assignee: Takoda Pharmaceutical Company LimitedInventors: Isao Aoki, Mari Adachi, Hiroyuki Tawada, Makoto Yamashita, Misayo Sera
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Patent number: 7420068Abstract: The present invention discloses crystalline particles of escitalopram oxalate which either have a broad particle size distribution or comprise at least 0.01% (w/w) of Z-4-(4-dimethylamino-1-(4-fluorophenyl)-but-1-enyl)-3-hydroxymethyl-benzonitrile, said particles being suitable for use in direct compression. Furthermore, the invention discloses a novel pharmaceutical unit dosage form containing such crystalline particles of escitalopram oxalate as well as methods for manufacture of such crystalline particles of escitalopram oxalate Finally, the invention provides a method for reduction of the amount of hydroxyl containing impurities in a solution of citalopram or escitalopram.Type: GrantFiled: September 23, 2004Date of Patent: September 2, 2008Assignee: H. Lundbeck A/SInventors: Kim Bojstrup Jensen, Rikke Eva Humble, Ken Liljegren, Troels Volsgaard Christensen
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Patent number: 7420001Abstract: The present invention relates to biaryl sulfonamides and their use as, for example, metalloproteinase inhibitors.Type: GrantFiled: December 1, 2004Date of Patent: September 2, 2008Assignee: WyethInventors: Jeremy Ian Levin, Thomas Saltmarsh Rush, III, Frank Lovering, Yonghan Hu, Jianchang Li, Wei Li, Jun Jun Wu, Rajeev Hotchandani, Jason Shaoyun Xiang, Xuemei Du, Derek Cecil Cole, Steve Yikkai Tam
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Publication number: 20080200540Abstract: The present invention relates to compounds of the formula (I) and pharmaceutically acceptable salts thereof, compositions containing such compounds and the uses of such compounds as antiparasitic agents.Type: ApplicationFiled: February 20, 2008Publication date: August 21, 2008Applicant: PFIZER LIMITEDInventors: Stephen Paul Gibson, Christelle Lauret
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Patent number: 7411077Abstract: A process for the preparation of citalopram and the pharmaceutically acceptable salts therof is disclosed by reacting 5-cyanophthalide with a 4-fluorophenyl magnesium halide, reducing the 3-hydroxymethyl-4-(4-fluorobenzoyl)benzonitrile with an agent reducing ketones to alcohols, submitting the thus-obtained 3-hydroxymethyl-4-[(4-fluorophenyl)hydroxymethyl)benzonitrile to a cyclization reaction to give 1-(4-fluorophenyl)-1,3-dihydro-5-isobenzofurancarbonitrile without 1,1-bis(4-fluorophenyl)-1,3-dihydro-5-isobenzofurancarbonitrile and treating 1,1-bis(4 fluorophenyl)-1,3-dihydro-5-isobenzofurancarbonitrile with a 3-(dimetylamino)propyl halide in the presence of a base.Type: GrantFiled: March 9, 2004Date of Patent: August 12, 2008Assignee: Adorken Technology SpAInventors: Giovanni Cotticelli, Leone Dall'Asta, Gianluca Di Lernia
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Patent number: 7405311Abstract: This invention provides a class of therapeutic compounds and methods for the treatment of mammals with physiological disorders, such as for example a frequently occurring type of essential hypertension, which are critically associated with the decreased binding of magnesium to the plasma membranes of their cells. These methods consist of administering to a mammal in need of such treatment a compound selected from a series of disubstituted trans, trans 1,3-butadienes, 1,3-disubstituted perhydrobutadienes, 1,2-disubstituted trans ethylenes and 1,2 disubstituted ethanes and disubstituted propanes, each of which embodies, in common, the unique structural feature essential for the biological activity of these compounds. This invention also provides for pharmaceutical formulations that employ these novel compounds.Type: GrantFiled: March 28, 2007Date of Patent: July 29, 2008Assignee: Magnesium Diagnostics, Inc.Inventor: Ibert Clifton Wells
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Publication number: 20080177096Abstract: The present invention provides a process for preparation of 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-5-isobenzofuran car-bonitrile comprising reacting a compound of formula IVa, in the presence of a base with a compound of formula RX, wherein R is selected from alkyl, alkenyl, aryl and heteroaryl which may be optionally substituted with electron withdrawing groups and X is selected from F, Cl, Br, I, CN, OTf and OR1, wherein Tf represents trifluoromethanesulfonyl group, and R1 is optionally substituted alkyl, Z is a cyano group or a group that may be converted to a cyano group; further wherein RX is selected such that an intermediate ether derivative, a compound of formula Va formed from said reaction cyclizes to a compound of formula VI, and where Z is not a cyano group, conversion of the group Z in the compound of formula VI to a cyano group to form 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-5-isobenzofuran carbonitrile.Type: ApplicationFiled: February 1, 2008Publication date: July 24, 2008Applicant: Sun Pharmaceutical Industries Ltd.Inventors: Periyandi Nagarajan, Kilaru Srinivasu, Thennati Rajamannar
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Patent number: 7402687Abstract: Compounds of formula I are described herein which are agonists or partial agonists of the 2C subtype of brain serotonin receptors. or pharmaceutically acceptable salts thereof, wherein each of R1, R2, R3, R4, Rx, Ry, and n are as defined herein. Such compounds, and compositions thereof, are useful for treating a variety of central nervous system disorders such as schizophrenia.Type: GrantFiled: April 21, 2006Date of Patent: July 22, 2008Assignee: WyethInventors: Gary Paul Stack, Jianyao Wang, William Demaio, Ronald Jordan, John Chuck Lem Erve, Rasmy Elsayed Talaat, Matthew John Hoffmann
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Patent number: 7396857Abstract: Therapeutic combinations useful in the treatment or prevention of depression or other mood disorders, to pharmaceutical compositions containing said combinations, and to their use in the treatment or prophylaxis of depression or other mood disorders are provided. Such compounds are of formula I: or a pharmaceutically acceptable salt thereof, wherein each of R1, R2, R3, n, y, and Ar are as defined and described herein.Type: GrantFiled: April 21, 2006Date of Patent: July 8, 2008Assignee: WyethInventors: Janet Jandura, Sharon Rosenzweig-Lipson
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Publication number: 20080161388Abstract: The present invention relates to the crystalline base of the well known antidepressant drug escitalopram, S-1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-5-isobenzo-furancarbonitrile, formulations of said base, a process for the preparation of purified salts of escitalopram, such as the oxalate, using the base, the salts obtained by said process and formulations containing such salts, and a process for the preparation of purified escitalopram free base or salts of escitalopram, such as the oxalate, using the hydrobromide, the salts obtained by said process and formulations containing such salts. Finally the present invention relates to an orodispersible tablet having a hardness of at least 22 N and an oral-disintegration time of less than 120 s and comprising an active pharmaceutical ingredient adsorbed onto a water soluble filler wherein the active pharmaceutical ingredient has a melting point in the range of 40-100° C., as well as a method for making such an orodispersible tablet.Type: ApplicationFiled: March 12, 2008Publication date: July 3, 2008Applicant: H. LUNDBECK A/SInventors: Robert Dancer, Hans Petersen, Ole Nielsen, Michael Harold Rock, Helle Eliasen, Ken Liljegren
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Publication number: 20080139547Abstract: The present invention is directed to certain hydroxamate derivatives that are inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.Type: ApplicationFiled: February 7, 2008Publication date: June 12, 2008Applicant: PHARMACYCLICS, INC.Inventor: Martin SENDZIK
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Publication number: 20080119662Abstract: A process for one pot synthesis of citalopram is disclosed. The process comprises subjecting 5-cyano phthalide to Grignard reduction followed cyclization and followed by C-alkylation reaction to obtain citalopram without isolation and purification of any intermediates. In another embodiment, 5-cyano phthalide is subjected to sequential Grignard reactions followed by cyclization to obtain citalopram without isolation and purification of any intermediate stages.Type: ApplicationFiled: February 16, 2004Publication date: May 22, 2008Applicant: Jubilant Organosys LimtedInventors: Ambati Narahari Babu, Vuddamari Srinivas Goud, Santosh Laxman Gaonkar, Sulur G. Manjunatha, Ashok Krishna Kulkarni, Madhari A. Kulkarni
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Patent number: 7368477Abstract: Compounds of formula I or pharmaceutically acceptable salts thereof are provided: wherein each of R1, R1?, R2, R3, R4, n, and Ar are as defined, and described in classes and subclasses herein, which are agonists or partial agonists of the 2C subtype of brain serotonin receptors. The compounds, and compositions containing the compounds, can be used to treat a variety of central nervous system disorders such as schizophrenia.Type: GrantFiled: April 21, 2006Date of Patent: May 6, 2008Assignee: WyethInventors: Jonathan Laird Gross, Gary Paul Stack, Dahui Zhou, Hong Gao
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Patent number: 7365216Abstract: The invention relates to a process for the manufacture of salts of citalopram in high purity. By the careful selection of solvents and the careful manipulation of the pH value, citalopram salts may be isolated in the absence of 5-chlorocitalopram, 5-bromocitalo-pram, desmethyl-citalopram and 5-carobxyamide citalopram.Type: GrantFiled: April 18, 2002Date of Patent: April 29, 2008Assignee: Matrix Laboratories LimitedInventors: Jyothi Basu Abbineni, Hari Babu Bodepudi, Satyanarayana Chava, Venkata Ramana Rao Chunchu
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Patent number: 7364823Abstract: An amine compound represented by the following general formula (1) is incorporated as a charge-transporting substance into a charge-transporting layer of an electrophotographic photoreceptor.Type: GrantFiled: March 30, 2005Date of Patent: April 29, 2008Assignee: Sharp Kabushiki KaishaInventors: Akihiro Kondoh, Takatsugu Obata
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Patent number: 7351735Abstract: This invention relates to novel benzofuran and benzothiophene derivatives of the general table formula and their use for the treatment of hyper-proliferative disordersType: GrantFiled: February 21, 2003Date of Patent: April 1, 2008Assignee: Bayer Pharmaceuticals CorporationInventors: Chengzhi Zhang, Michael Burke, Zhi Chen, Jacques Dumas, Dongping Fan, Jianmei Fan, Holia Hatoum-Mokdad, Benjamin D. Jones, Gaetan Ladouceur, Wendy Lee, Barton Phillips
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Patent number: 7351842Abstract: The subject invention provides novel compounds for treatment of cardiac arrhythmia and methods of use.Type: GrantFiled: June 12, 2006Date of Patent: April 1, 2008Assignee: ARYx Therapeutics, Inc.Inventor: Pascal Druzgala
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Patent number: 7339078Abstract: Selected bis-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, compositions, and methods for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.Type: GrantFiled: August 10, 2006Date of Patent: March 4, 2008Assignee: G.D. Searle LLCInventors: Daniel P Getman, Gary A DeCrescenzo, John N Freskos, Michael L Vazquez, James A Sikorski, Balekudru Devadas, Srinivasan Raj Nagarajan, David L Brown, Joseph J McDonald
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Patent number: 7332518Abstract: The invention concerns novel carboxamides of formula (I) wherein A is (A1), (A2), (A3), (A4), (A5); Q is (Q1), (Q2), (Q3), (Q4), (Q5), (Q6); R1 is CH2 R2, CH2CH?CHR2, CH?C?CHR2 or COR3; R2 is hydrogen, C1-C6alkyl, C1-C6haloalkyl, C2-C6alkenyl, C2-C6alkynyl, C3-C7cycloalkyl, COOC1-C4alkyl, COOC3-C6alkenyl, COOC3-C6alkynyl or CN; R3 is C1-C6alkyl, C1-C6alkyl substituted by halogen, C1-C6alkoxy or C1-C6haloalkoxy; or is C1-C6alkylthio, C1-C6haloalkylthio, C1-C6alkoxy, C1-C6haloalkoxy; C3-C6alkenyloxy or C3-C6haloalkenyloxy; C3-C6haloalkenyloxy; C3-C6alkynyloxy or C3-C6haloalkynyloxy; R4 is methyl, CF2Cl, CF3, CF2H, CFH2, Cl or Br, R5 is methyl, CF3, CH2OCH3 or CH2OCF3; R6 is hydrogen, fluoro, CF3 or methyl; R7 is hydrogen, methyl or halogen; and Z is phenyl, halophenyl, C5-C7cycloalkyl, C5-C7cycloalkyl substituted by C1-C3alkyl, C1C3haloalkyl or halogen, or a group of the form —CHR8—CH2—CHR9R10 wherein R8, R9 and R10 are independently of each other C1-C3alkyl.Type: GrantFiled: January 24, 2002Date of Patent: February 19, 2008Assignee: Syngenta Crop Protection, Inc.Inventors: Harald Walter, Stephan Trah
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Patent number: 7276612Abstract: The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.Type: GrantFiled: April 6, 2004Date of Patent: October 2, 2007Assignee: Pharmacyclics, Inc.Inventors: Eric J. Verner, Martin Sendzik, Chitra Baskaran, Joseph J. Buggy, James Robinson
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Patent number: 7273886Abstract: Compounds of Formula I are useful for inhibiting serine protease enzymes, such as TF/factor VIIa, factor Xa, thrombin and kallikrein and have improved pharmacokinetic properties. These compounds may be used in methods of preventing and/or treating clotting disorders.Type: GrantFiled: May 19, 2004Date of Patent: September 25, 2007Assignee: Genentech, Inc.Inventors: Alan G. Olivero, Daniel P. Sutherlin