The Six-membered Hetero Ring Shares Ring Members With One Other Cyclo Only Patents (Class 546/77)
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Patent number: 11690290Abstract: A novel organic compound is provided. An organic compound represented by General Formula (G1) is provided. In General Formula (G1), A represents a substituent including a hole-transport skeleton, L1 represents any one of a single bond, a substituted or unsubstituted phenylene group, and a substituted or unsubstituted biphenyldiyl group, R1 and R2 independently represent any one of hydrogen and an alkyl group having 1 to 6 carbon atoms, any one of Ar1 to Ar4 is a group represented by General Formula (g1), and the others independently represent any one of hydrogen and an alkyl group having 1 to 6 carbon atoms. In General Formula (g1), B represents any one of a substituted or unsubstituted carbazolyl group, a substituted or unsubstituted dibenzofuranyl group, a substituted or unsubstituted dibenzothiophenyl group, and a substituted or unsubstituted triphenylenyl group, and L2 represents a substituted or unsubstituted phenylene group or a substituted or unsubstituted biphenyldiyl group.Type: GrantFiled: August 4, 2020Date of Patent: June 27, 2023Assignee: Semiconductor Energy Laboratory Co., Ltd.Inventors: Tomoka Hara, Hideko Yoshizumi, Hiromitsu Kido, Satoshi Seo
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Patent number: 9035042Abstract: The invention concerns the production of quinoline compounds containing sulfonic acid groups, the said quinoline compounds and their conversion into dyes containing sulfonic acid groups. The dyes according to the invention are used especially to label analytes, for example to label biomolecules.Type: GrantFiled: July 2, 2004Date of Patent: May 19, 2015Assignee: ATTO-TEC GmbHInventors: Alexander Zilles, Jutta Arden-Jacob, Karl-Heinz Drexhage, Norbert Uwe Kemnitzer, Monika Hamers-Schneider
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Publication number: 20150064168Abstract: Cadherin-11 inhibitors and methods for the prevention and treatment of cadherin-11 related diseases are described herein. Cadherin-11 related diseases include cancer and rheumatoid arthritis.Type: ApplicationFiled: July 3, 2014Publication date: March 5, 2015Inventors: Stephen W. Byers, Sivanesan Dakshanamurthy, Jaime M. Guidry Auvil, Milton L. Brown
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Publication number: 20150060824Abstract: Provided is a novel organic compound that is used as a host material in which a light-emitting substance is dispersed. The organic compound is represented by General Formula (G1). In the formula, A represents a substituted or unsubstituted dibenzofuran-diyl group, a substituted or unsubstituted dibenzothiophene-diyl group, a substituted or unsubstituted N-aryl-9H-carbazole-diyl group, or a substituted or unsubstituted N-alkyl-9H-carbazole-diyl group; Ar1 and Ar2 each independently represent a single-bond or a substituted or unsubstituted arylene group; R11 to R19 and R21 to R29 each independently represent hydrogen, an alkyl group having 1 to 6 carbon atoms, or a substituted or unsubstituted aryl group having 6 to 13 carbon atoms; X1 and X2 each independently represent a carbon atom or a nitrogen atom; and the carbon atom is bonded to hydrogen, an alkyl group having 1 to 6 carbon atoms, or a substituted or unsubstituted aryl group having 6 to 13 carbon atoms.Type: ApplicationFiled: August 29, 2014Publication date: March 5, 2015Inventors: Yoshimi Ishiguro, Sachiko KAWAKAMI, Hiromi SEO, Tatsuyoshi TAKAHASHI, Satoshi SEO
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Publication number: 20140332758Abstract: Donor-acceptor compounds with nitrogen containing polyaromatics as the acceptor with emission originated from the charge transfer (CT) state is disclosed. The donor-acceptor compound is provided that has the structure of Formula 1 shown below: wherein X1 to X12 is independently selected from the group consisting of C—R and N, wherein at least one of X1 to X12 is N, wherein each R is independently selected from the group consisting of hydrogen, deuterium, halide, alkyl, cycloalkyl, heteroalkyl, arylalkyl, alkoxy, aryloxy, amino, silyl, alkenyl, cycloalkenyl, heteroalkenyl, alkynyl, aryl, heteroaryl, acyl, carbonyl, carboxylic acids, ester, nitrile, isonitrile, sulfanyl, sulfinyl, sulfonyl, phosphino, and combinations thereof; and at least one of the R comprises a donor group with at least two electron-donating nitrogens.Type: ApplicationFiled: May 9, 2013Publication date: November 13, 2014Applicant: UNIVERSAL DISPLAY CORPORATIONInventors: Raymond Kwong, Sui Tung Lam, Chi Hang Lee
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Patent number: 8846924Abstract: The invention concerns the production of quinoline compounds containing sulfonic acid groups, the said quinoline compounds and their conversion into dyes containing sulfonic acid groups. The dyes according to the invention are used especially to label analytes, for example to label biomolecules.Type: GrantFiled: March 25, 2011Date of Patent: September 30, 2014Assignee: Atto-Tec GmbHInventors: Alexander Zilles, Jutta Arden-Jacob, Karl-Heinz Drexhage, Norbert Uwe Kemnitzer, Monika Hamers-Schneider
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Publication number: 20140183503Abstract: Disclosed is a light-emitting element having high emission efficiency, capable of driving at low voltage, and showing a long lifetime. The light-emitting element contains a compound between a pair of electrodes, and the compound is configured to give a first peak of m/z around 202 and a second peak of m/z around 227 in a mass spectrum. The first and second peaks are product ions of the compound and possess compositions of C16H9 and C17H10N, respectively, which are derived from a dibenzo[f,h]quinoline unit.Type: ApplicationFiled: December 27, 2013Publication date: July 3, 2014Applicant: Semiconductor Energy Laboratory Co., Ltd.Inventors: Hiroshi Kadoma, Kaori Ogita, Satoko Shitagaki, Nobuharu Ohsawa, Satoshi Seo, Harue Osaka
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Patent number: 8664396Abstract: A method of staining a poly(amino acid) by contacting a poly(amino acid) with an overall neutral or overall cationic complex of at least one of transition metal ion, and a plurality of donor ligands each of which is fully coordinated to the transition metal ion and is either a nitrogen donor ligand or a cyclometalated donor ligand, such that at least one of the donor ligands is a cyclometalated donor ligand. Nitrogen donor ligands will contain heteroaryl ring systems having from 10 to 40 ring atoms, wherein each nitrogen donor ligand is substituted with from 0 to 4 R1 groups. Cyclometalated donor ligands will likewise contain heteroaryl ring systems having from 10 to 40 ring atoms, such that at least one ring atom is N, wherein each cyclometalated donor ligand is substituted with from 0 to 4 R1 groups. R1, R2, R3 and R4 groups are defined herein.Type: GrantFiled: November 20, 2008Date of Patent: March 4, 2014Assignee: Bio-Rad Laboratories, Inc.Inventor: Tom Berkelman
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Patent number: 8664395Abstract: The present invention relates to a process of separation of 4-aza-androst-1-ene-17-oic acid from 4-aza-androstan-17-oic acid, which brings to 4-aza-androst-1-ene-17-oic containing less than 0.05% w/w of 4-aza-androstan-17-oic acid, with high yield and productivity. In particular, the present invention relates to a process for the separation of 4-aza-androstan-17-oic acid from 4-aza-androst-1-ene-17-oic acid, comprising the steps of treating the crude 4-aza-androst-1-ene-17-oic acid with formic acid and recovering the purified 4-aza-androst-1-ene-17-oic acid containing 4-aza-androstan-17-oic acid in w/w % less than 0.05%.Type: GrantFiled: April 2, 2009Date of Patent: March 4, 2014Assignee: PHF S.A.Inventors: Mauro Bonetti, Sabrina De Rosa
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Patent number: 8614317Abstract: The invention concerns the production of quinoline compounds containing sulfonic acid groups, the said quinoline compounds and their conversion into dyes containing sulfonic acid groups. The dyes according to the invention are used especially to label analytes, for example to label biomolecules.Type: GrantFiled: March 25, 2011Date of Patent: December 24, 2013Assignee: Atto-Tec GmbHInventors: Alexander Zilles, Jutta Arden-Jacob, Karl-Heinz Drexhage, Norbert Uwe Kemnitzer, Monika Hamers-Schneider
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Patent number: 8592416Abstract: There are provided substituted isoquinolin-1(2H)-one derivatives which selectively inhibit the activity of poly (ADP-ribose) polymerase PARP-1 with respect to poly (ADP-ribose) polymerase PARP-2. The compounds of the present invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds. A screening method for the identification of compounds capable of binding several PARP proteins, as well the probes used in such method, are further objects of the invention.Type: GrantFiled: May 19, 2010Date of Patent: November 26, 2013Assignee: Nerviano Medical Sciences S.r.l.Inventors: Gianluca Mariano Enrico Papeo, Jay Aaron Bertrand, Giovanni Cervi, Barbara Forte, Rosita Lupi, Alessia Montagnoli, Alessandra Scolaro, Fabio Zuccotto, Paolo Orsini, Helena Posteri
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Publication number: 20130292653Abstract: Embodiments of the present invention are directed to a condensed-cyclic compound represented by Formula 1, and to an organic light-emitting diode including the same.Type: ApplicationFiled: November 27, 2012Publication date: November 7, 2013Applicant: Samsung Display Co. Ltd.Inventors: Bum-Woo Park, Yoon-Hyun Kwak, Sun-Young Lee, Se-Jin Cho
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Patent number: 8569331Abstract: The present invention relates to substituted benzo[f]imidazo[1,2-d]pyrido[2,3-b][1,4]diazepine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted benzo[f]imidazo[1,2-d]pyrido[2,3-b][1,4]diazepine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.Type: GrantFiled: November 1, 2011Date of Patent: October 29, 2013Assignee: ArQule, Inc.Inventors: Mark A. Ashwell, Sudharshan Eathiraj, Anton Filikov, Steffi Koerner, Jean-Marc Lapierre, Yanbin Liu, Rocio Palma, David Vensel, Shin Iimura, Akiko Shiina, Kenichi Yoshida, Takanori Yamazaki, Akihisa Matsuda
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Patent number: 8563728Abstract: The present invention provides an improved process for the preparation of Dutasteride (I) which comprises: (i) reacting 4-aza-5?-androst-1-en-3-one-17?-carboxylic acid (VII), Formula VII with sulfonic acid anhydride (RSO2)2O in presence of base to produce an intermediate compound of Formula (XIII), wherein R represents C1-6 alkyl, C1-6 halo alkyl, C6-10 aryl, halo aryl; (ii) condensing compound of Formula (XIII) with 2,5-bis(trifluoromethyl)aniline (III), Formula (III) in the presence or absence of a base to produce Dutasteride (I).Type: GrantFiled: July 7, 2010Date of Patent: October 22, 2013Assignee: Aurobindo Pharma Ltd.Inventors: Sambhu Prasad Sarma Mallela, Sukumar Nandi, Balanarasimha Reddy Gona, Naresh Akkina, Rani Ananta, Islam Aminul, Sivakumaran Meenakshisunderam
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Publication number: 20130224871Abstract: The present invention relates to polycyclic compounds of the general formula (I) which are distinguished by an amine substituent NR6R7 on the central carbon atom of the chromophore, to processes for their preparation, and to the use thereof for the determination of analytes.Type: ApplicationFiled: October 18, 2011Publication date: August 29, 2013Applicant: ATTO-TEC GmbHInventors: Alexander Zilles, Karl-Heinz Drexhage, Norbert Uwe Kemnitzer, Jutta Arden-Jacob, Monika Hamers-Schneider
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Patent number: 8415347Abstract: This invention concerns novel substituted tetracyclic tetrahydrofuran, pyrrolidine and tetrahydrothiophene derivatives with binding affinities towards serotonin receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.Type: GrantFiled: August 5, 2010Date of Patent: April 9, 2013Assignee: Janssen Pharmaceutica, NVInventors: José Maria Cid-Núñez, Antonius Adrianus Hendrikus Petrus Megens, Andrés Avelino Trabanco-Suárez, Mohamed Koukni, Georges Joseph Cornelius Hoornaert, Frans Josef Cornelius Compernolle, Tomasz Kozlecki, Hua Mao, Sushil Chandra Jha, Francisco Javier Fernández-Gadea
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Publication number: 20130009543Abstract: Provided is a novel heterocyclic compound which can be used as a host material for dispersing a light-emitting material in a light-emitting layer of a light-emitting element. Further provided is a light-emitting element which is driven at a low voltage and has high current efficiency. By including the light-emitting element, a light-emitting device, an electronic device, and a lighting device each with reduced power consumption are provided. The light-emitting element contains a compound in which a dibenzo[f,h]quinoline ring and a hole-transport skeleton are bonded through an arylene group. The light-emitting device, the electronic device, and the lighting device each including the light-emitting element are provided. The light-emitting element contains a heterocyclic compound having a structure represented by the following general formula (G1).Type: ApplicationFiled: June 29, 2012Publication date: January 10, 2013Applicant: SEMICONDUCTOR ENERGY LABORATORY CO., LTD.Inventors: Hiroshi Kadoma, Kaori Ogita, Satoko Shitagaki, Nobuharu Ohsawa, Satoshi Seo
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Publication number: 20130001527Abstract: Provided are a heterocyclic compound represented by Formula 1 below, and an organic light-emitting diode and a flat display device each including the heterocyclic compound. The organic light-emitting diode including an organic layer including the heterocyclic compound has a low driving voltage, high luminescence efficiency, and long lifetime.Type: ApplicationFiled: January 30, 2012Publication date: January 3, 2013Applicant: SAMSUNG MOBILE DISPLAY CO., LTD.Inventors: Sang-Hyun Han, Seok-Hwan Hwang, Young-Kook Kim, Hye-Jin Jung, Jin-O Lim, Se-Jin Cho, Jong-Hyuk Lee
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Publication number: 20130001522Abstract: A heterocyclic compound represented by Formula 1 below and an organic light-emitting device including the same: wherein Formula 1 is defined as in the detailed description.Type: ApplicationFiled: October 13, 2011Publication date: January 3, 2013Applicant: SAMSUNG MOBILE DISPLAY CO., LTD.Inventors: Sun-Young Lee, Yoon-Hyun Kwak, Bum-Woo Park, Hee-Joo Ko, Jong-Hyuk Lee
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Publication number: 20120319087Abstract: A heterocyclic compound, organic light-emitting device, and a flat panel display device, the heterocyclic compound being represented by Formula 1 or 2 below:Type: ApplicationFiled: December 15, 2011Publication date: December 20, 2012Inventors: Sun-Young Lee, Seok-Hwan Hwang, Young-Kook Kim, Yoon-Hyun Kwak, Hye-Jin Jung, Jin-O Lim, Jong-Hyuk Lee, Sang-Hyun Han, Se-Jin Cho
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Publication number: 20120226044Abstract: A process for the preparation of 4-steroids of the formula: R1 and R2 are independently selected from the group that is hydrogen, F, Cl, Br, I, C1-6-allyl and C1-6-alkoxy, and R4 is selected from the group that is hydrogen, (N,N-di-C1-6-allylamino)methyl, allylamino)ethyl, C1-6-alkyl, C1-6-alkoxy, phenyl and benzyl, and Q7 represents a carbonyl oxygen atom or is R7-1 and R7-2, wherein one of R7-1 and R7-2 is hydrogen and the other is selected from the group that is hydrogen, F, Cl, Br, I, C1-6-alkyl and C1-6-alkoxy, and R9 represents hydrogen or F, and Q11 represents a carbonyl oxygen atom or is R11-1 and R11-2, wherein one of R11-1 and R11-2 is hydrogen and the other is selected from the group that is hydrogen, cyano, cyano-C1-3-alkyl, acetoxy, COOH and COO?M+, wherein M+ is Na+, K+ or NH+4, and R16 is selected from the group that is hydrogen, cyano, cyano-C1-3-alkyl, acetoxy, COOH and COO?M+, wherein M+ is Na+, K+ or NH+4, and COOR represents COOH or COO?M+, wherein M+ is Na+, K+ or NH+4.Type: ApplicationFiled: July 4, 2005Publication date: September 6, 2012Inventors: Yves Bessard, David L. Kuo
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Publication number: 20120157454Abstract: There are provided substituted isoquinolin-1(2H)-one derivatives which selectively inhibit the activity of poly (ADP-ribose) polymerase PARP-1 with respect to poly (ADP-ribose) polymerase PARP-2. The compounds of the present invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds. A screening method for the identification of compounds capable of binding several PARP proteins, as well the probes used in such method, are further objects of the invention.Type: ApplicationFiled: May 19, 2010Publication date: June 21, 2012Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Gianluca Mariano Enrico Papeo, Jay Aaron Bertrand, Giovanni Cervi, Barbara Forte, Rosita Lupi, Alessia Montagnoli, Alessandra Scolaro, Fabio Zuccotto, Paolo Orsini, Helena Posteri
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Publication number: 20120153269Abstract: An organic light-emitting device includes an anode, a cathode, and an organic compound layer interposed between the anode and the cathode. The organic compound layer contains a heterocyclic compound having 4,10-Diazachrysene.Type: ApplicationFiled: August 4, 2010Publication date: June 21, 2012Applicant: CANON KABUSHIKI KAISHAInventors: Takayuki Horiuchi, Jun Kamatani, Akihito Saitoh
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Publication number: 20120157683Abstract: The present invention provides an improved process for the preparation of Dutasteride (I) which comprises: (i) reacting 4-aza-5?-androst-1-en-3-one-17?-carboxylic acid (VII), Formula VII with sulfonic acid anhydride (RSO2)2O in presence of base to produce an intermediate compound of Formula (XIII), wherein R represents C1-6 alkyl, C1-6 halo alkyl, C6-10 aryl, halo aryl; (ii) condensing compound of Formula (XIII) with 2,5-bis(trifluoromethyl)aniline (III), Formula (III) in the presence or absence of a base to produce Dutasteride (I).Type: ApplicationFiled: July 7, 2010Publication date: June 21, 2012Inventors: Sambhu Prasad Sarma Mallela, Sukumar Nandi, Balanarasimha Reddy Gona, Naresh Akkina, Rami Ananta, Islam Aminul, Sivakumaran Meenakshisunderam
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Publication number: 20120086329Abstract: Compounds comprising a 3,9-linked oligocarbazole moiety and a dibenzothiophene, dibenzofuran, dibenzoselenophene, aza-dibenzothiophene, aza-dibenzofuran, or aza-dibenzoselenophene are provided. The 3,9-linked oligocarbazole and dibenzo or aza-dibenzo moiety are separated by an aromatic spacer. The compounds may be used as non-emissive materials for phosphorescent OLEDs to provide devise having improved performance.Type: ApplicationFiled: October 8, 2010Publication date: April 12, 2012Applicant: Universal Disolay CorporationInventor: Alexey Dyatkin
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Patent number: 8153648Abstract: The solid state chemistry of 17?-N-[2,5-bis(trifluoromethyl)phenyl]carbamoyl-4-aza-5-?-androst-1-en-3-one of which the international nonproprietary name is Dutasteride (the active ingredient in products marketed as Avodart, Avidart, Avolve, Duagen, Dutas, Dutagen, Duprost) and its process for preparing. The synthetic process comprises formation of the mixed anhydride, its subsequent reaction with 2,5-bis(trifluoromethyl)phenylamine in the presence of an appropriate Lewis catalyst and its isolation, purification and crystallization from acetonitrile/water.Type: GrantFiled: January 3, 2009Date of Patent: April 10, 2012Assignee: Gador S.A.Inventors: Dora Graciela Tombari, Constanza Pia Mangone, Maria Beatriz Garcia, Adriana Vechhioli, Rafael Alberto Labriola
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Patent number: 8124614Abstract: There is provided a compound having Formula (I) wherein G is H or a substituent, and wherein R1 is any one of a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group, capable of inhibiting steroid sulphatase.Type: GrantFiled: September 14, 2007Date of Patent: February 28, 2012Assignee: Sterix LimitedInventors: Barry Victor Lloyd Potter, Michael John Reed, Lok Wai Lawrence Woo
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Publication number: 20120029196Abstract: The present invention relates to a process of separation of 4-aza-androst-1-ene-17-oic acid from 4-aza-androstan-17-oic acid, which brings to 4-aza-androst-1-ene-17-oic containing less than 0.05% w/w of 4-aza-androstan-17-oic acid, with high yield and productivity. In particular, the present invention relates to a process for the separation of 4-aza-androstan-17-oic acid from 4-aza-androst-1-ene-17-oic acid, comprising the steps of treating the crude 4-aza-androst-1-ene-17-oic acid with formic acid and recovering the purified 4-aza-androst-1-ene-17-oic acid containing 4-aza-androstan-17-oic acid in w/w % less than 0.05%.Type: ApplicationFiled: April 2, 2009Publication date: February 2, 2012Applicant: PHF S.A.Inventors: Mauro Bonetti, Sabrina De Rosa
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Patent number: 7998970Abstract: The present invention relates to new pharmaceutical uses of 4-azasteroid compounds, in particular of Finasteride/Dutasteride/Dutasteride and Dutasteride, particularly preferred of Finasteride/Dutasteride/Dutasteride, and its pharmaceutically acceptable derivatives, and combinations comprising said compounds. The invention also features generally the use of a modulator compound of neuroprotective conditions via beta subunits of shaker-type voltage-gated potassium channels and/or via members of solute carriers family 25, in particular Aralar (member 12) and adenine-nucleotide translocators 1 & 2 (member 4 & 5) and/or via a 4-nitrophenylphosphatase domain and non-neuronal SNAP25-like protein homolog 1 (NIPSNAP 1) as a neuroprotective medicament, particularly as a medicament for the prevention and/or treatment of neurological diseases such as dementia, Parkinson, Alzheimer, schizophrenia or epilepsy.Type: GrantFiled: December 2, 2005Date of Patent: August 16, 2011Assignee: ProteoSys AGInventors: Vukic Soskic, André Schrattenholz
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Publication number: 20110190486Abstract: The invention concerns the production of quinoline compounds containing sulfonic acid groups, the said quinoline compounds and their conversion into dyes containing sulfonic acid groups. The dyes according to the invention are used especially to label analytes, for example to label biomolecules.Type: ApplicationFiled: March 25, 2011Publication date: August 4, 2011Applicant: ATTO-TEC GMBHInventors: Alexander Zilles, Jutta Arden-Jacob, Karl-Heinz Drexhage, Norbert Uwe Kemnitzer, Monika Hamers-Schneider
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Patent number: 7989089Abstract: The invention provides organic compounds of the general structure (1) that are photoluminescent and electroluminescent, emitting intense blue light. The invention further provides methods of synthesizing such compounds, methods of producing photoluminescence and electroluminescence, methods of applying the compounds in thin films, and uses of the compounds of the invention in luminescent probes, electroluminescent displays and as pH probes and metal ion detectors.Type: GrantFiled: April 16, 2004Date of Patent: August 2, 2011Assignee: LG Display Co., Ltd.Inventors: Suning Wang, Ruiyao Wang
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Publication number: 20110178065Abstract: Provided herein are inhibitors of CYP17 enzyme. Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat androgen-dependent diseases, disorders and conditions.Type: ApplicationFiled: January 13, 2011Publication date: July 21, 2011Applicant: BIOMARIN PHARMACEUTICAL INC.Inventors: Daniel Chu, Bing Wang, Tao Ye
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Publication number: 20110059948Abstract: The invention relates to a compound of general formula I, II, III, IV, V, VI, VII, VIII, IX, X or a tautomer and the stereochemically isomeric forms thereof or pharmaceutically acceptable salts thereof, a N-oxide form thereof or a pro-drug thereof. The compound is usable as a medicament for the treatment of mycobacterial disease.Type: ApplicationFiled: January 9, 2009Publication date: March 10, 2011Inventors: Jyoti Chattopadhyaya, Ram Shankar Upadhayaya
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Publication number: 20110015164Abstract: A method of safely and specifically treating the combined metabolic disturbances of insulin resistance and visceral adiposity in male subject with visceral adiposity, metabolic syndrome (also known as the ‘insulin resistance syndrome’, and ‘syndrome X’), type II diabetes, or insulin resistance by administering a 5-alpha reductase inhibiting compound of structural formula I, II, III, or IV is disclosed. The method is also concerned with the use of the 5alpha reductase inhibiting compound together with antidiabetic agents, lipid lowering agents, antihypertensive agents, antiobesity agents, testosterone, testosterone precursors, testosterone prodrugs, testosterone analogs, and other androgen receptor agonists for treating visceral adiposity, metabolic syndrome, type II diabetes and insulin resistance in men.Type: ApplicationFiled: September 27, 2010Publication date: January 20, 2011Inventor: Alan Meehan
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Patent number: 7872135Abstract: A process for preparing 17?-substituted 4-azaandrost-1-en-3-one compounds of the general formula (I): or a pharmaceutically approved salt thereof, where R is hydroxyl, optionally substituted, linear or branched (C1-C2)alkyl or (C1-C12)alkenyl; phenyl or benzyl; an —OR1 radical, or an —NHR1 radical, or an —NR1R2 radical; R1 is hydrogen, optionally substituted, linear or branched (C1-C12)alkyl or (C1-C12)alkenyl, or optionally substituted phenyl; R2 is hydrogen, methyl, ethyl or propyl; or —NR1R2 is a 5- or 6-membered heterocyclic ring, by (A) introducing protecting groups into the 3-keto-4-aza moiety of the corresponding 1,2-dihydro compound, so that a compound of the general formula (III) is formed: where R3 is trialkylsilyl or, together with R4, the —C(O)—C(O)— or —C(O)—Y—C(O)— radical; R4 is alkyloxycarbonyl or phenyloxycarbonyl, preferably Boc (=tert-butyloxycarbonyl); or trialkylsilyl, or, together with R3, the —C(O)—C(O)— or —C(O)—Y—C(O)— radical; Y is —[C(R5)(R6)]n— or —CH(R5)?CH(R6)—, or ortType: GrantFiled: July 2, 2003Date of Patent: January 18, 2011Assignee: Siegfried Ltd.Inventors: Norber Schärer, Beat Webber, Beat W Müller
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Publication number: 20100331325Abstract: This invention concerns novel substituted tetracyclic tetrahydrofuran, pyrrolidine and tetrahydrothiophene derivatives with binding affinities towards serotonin receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.Type: ApplicationFiled: August 5, 2010Publication date: December 30, 2010Inventors: José Maria CID-NÚÑEZ, Antonius Adrianus Hendrikus Petrus MEGENS, Andrés Avelino TRABANCO-SUÁREZ, Mohamed KOUKNI, Georges Joseph Cornelius HOORNAERT, Frans Josef Cornelius COMPERNOLLE, Tomasz KOZLECKI, Hua MAO, Sushil Chandra JHA, Francisco Javier FERNÁNDEZ-GADEA
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Publication number: 20100289406Abstract: Compounds containing 2-azatriphenylene are provided. In particular, compounds containing a 2-azatriphenylene core having an additional aromatic group are provided. The compounds provided may be emissive or non-emissive materials. The compounds may be used in organic light emitting devices, particularly as host materials, hole blocking layer materials, or emitting dopants. Devices comprising 2-azatriphenylene containing compounds may demonstrate improved stability and efficiency.Type: ApplicationFiled: May 12, 2010Publication date: November 18, 2010Applicant: Universal Display CorporationInventors: Bin MA, Raymond C. Kwong
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Patent number: 7625919Abstract: Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner. They are useful as agonists of the androgen receptor in bone and/or muscle tissue while antagonizing the AR in the prostate of a male patient or in the uterus of a female patient.Type: GrantFiled: August 14, 2006Date of Patent: December 1, 2009Assignee: Merck & Co., Inc.Inventors: Jiabing Wang, Carol A. McVean
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Patent number: 7625920Abstract: Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner. They are useful as agonists of the androgen receptor in bone and/or muscle tissue while antagonizing the AR in the prostate of a male patient or in the uterus of a female patient. These compounds are therefore useful in the treatment of conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including osteoporosis, osteopenia, glucocorticoid-induced osteoporosis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, postmenopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, obesity, aplastic anemia and other hematopoietic disorders, inflammatory arthritis and joint repair, HIV-wasting, prostate cancer, cancer cachexia, muscular dystrophies, premature ovarian failure, and autoimmune disease, alone or in combination with other active agents.Type: GrantFiled: November 18, 2008Date of Patent: December 1, 2009Assignee: Merck & Co., Inc.Inventors: Robert S. Meissner, James J. Perkins
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Publication number: 20090170889Abstract: The present invention relates to new pharmaceutical uses of 4-azasteroid compounds, in particular of Finasteride/Dutasteride/Dutasteride and Dutasteride, particularly preferred of Finasteride/Dutasteride/Dutasteride, and its pharmaceutically acceptable derivatives, and combinations comprising said compounds. The invention also features generally the use of a modulator compound of neuroprotective conditions via beta subunits of shaker-type voltage-gated potassium channels and/or via members of solute carriers family 25, in particular Aralar (member 12) and adenine-nucleotide translocators 1 & 2 (member 4 & 5) and/or via a 4-nitrophenylphosphatase domain and non-neuronal SNAP25-like protein homolog 1 (NIPSNAP 1) as a neuroprotective medicament, particularly as a medicament for the prevention and/or treatment of neurological diseases such as dementia, Parkinson, Alzheimer, schizophrenia or epilepsy.Type: ApplicationFiled: December 2, 2005Publication date: July 2, 2009Applicant: PROTEOSYS AGInventors: Vukic Soskic, André Schrattenholz
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Patent number: 7550593Abstract: A process of preparing finasteride Form (I), which process comprises dissolving finasteride in a solvent, replacing the solvent partially or substantially completely with a nonsolvent and thereafter isolating finasteride Form (I). There is also provided finasteride Form (I) prepared in accordance with the present invention, and the therapeutic use thereof in the inhibition of 5-alpha reductase, and pharmaceutical compositions containing the same.Type: GrantFiled: July 5, 2004Date of Patent: June 23, 2009Assignee: Cipla LimitedInventors: Rajendra Narayanrao Kankan, Dharmaraj Ramachandra Rao
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Patent number: 7531658Abstract: The present invention relates to a process for producing 17-N-substituted-carbamoyl-4-aza-androst-1-en-3-ones of formula 1, including Finasteride and Dutasteride.Type: GrantFiled: January 20, 2006Date of Patent: May 12, 2009Assignee: Apotex Pharmachem Inc.Inventors: Zhi-Xian Wang, Alfredo Paul Ceccarelli, Mohammed Abdul Raheem, Bhaskar Reddy Guntoori
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Publication number: 20090076057Abstract: The present application describes deuterium-enriched dutasteride, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: August 22, 2008Publication date: March 19, 2009Applicant: Protia, LLCInventor: Anthony W. Czarnik
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Publication number: 20090076058Abstract: The present application describes deuterium-enriched finasteride, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: September 11, 2008Publication date: March 19, 2009Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
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Patent number: 7501515Abstract: The present invention relates to a novel polymorphic form of 17-?-(N-ter.butyl carbamoyl)-4-aza-5-?-androst-1-en-3-one (Finasteride) of the Formula (I) and processes for preparing the form.Type: GrantFiled: March 15, 2004Date of Patent: March 10, 2009Assignees: Dr. Reddy's Laboratories Limited, Dr. Reddy's Laboratories, Inc.Inventors: M. Satyanarayana Reddy, S. T. Rajan, M. V. N. Brahmeshwara Rao, K. Vyas, S. Vishnuvardhana Reddy, K. Shashi Rekha
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Publication number: 20090048283Abstract: The biphthalate salts of compound I are modulators of the androgen receptor (AR) in a tissue selective manner.Type: ApplicationFiled: August 12, 2008Publication date: February 19, 2009Inventor: Claire H. Lee
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Patent number: 7446110Abstract: Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner.Type: GrantFiled: September 2, 2004Date of Patent: November 4, 2008Assignee: Merck & Co., Inc.Inventors: Mildred L. Kaufman, Robert S. Meissner, Helen J. Mitchell
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Patent number: 7410977Abstract: Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner. These compounds are useful in the enhancement of weakened muscle tone and the treatment of conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including osteoporosis, osteopenia, glucocorticoid-induced osteoporosis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, postmenopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, obesity, aplastic anemia and other hematopoietic disorders, inflammatory arthritis and joint repair, HIV-wasting, prostate cancer, benign prostatic hyperplasia (BPH), cancer cachexia, Alzheimer's disease, muscular dystrophies, cognitive decline, sexual dysfunction, sleep apnea, depression, premature ovarian failure, and autoimmune disease, alone or in combination with other active agents.Type: GrantFiled: April 22, 2005Date of Patent: August 12, 2008Assignee: Merck & Co., Inc.Inventors: Robert S. Meissner, James J. Perkins
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Publication number: 20080122428Abstract: The present invention relates to a method of determining voltage changes, e.g. in cell membranes, by means of a voltage-sensitive dye.Type: ApplicationFiled: June 25, 2004Publication date: May 29, 2008Applicant: Max-Planck-Gesellschaft zur Forderungder Wissenschaften e. V.Inventors: Bernd Kuhn, Winfried Denk, Gerd Hubener, Peter Fromherz
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Publication number: 20080125399Abstract: Compounds of structural formula (I) are modulators of the androgen receptor (AR) in a tissue selective manner. These compounds are useful in the enhancement of weakened muscle tone and the treatment of conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including osteoporosis, osteopenia, glucocorticoid-induced osteoporosis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, postmenopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, obesity, aplastic anemia and other hematopoietic disorders, inflammatory arthritis and joint repair, HIV-wasting, prostate cancer, benign prostatic hyperplasia (BPH), cancer cachexia, Alzheimer's disease, muscular dystrophies, cognitive decline, sexual dysfunction, sleep apnea, depression, premature ovarian failure, and autoimmune disease, alone or in combination with other active agents.Type: ApplicationFiled: April 4, 2005Publication date: May 29, 2008Inventors: Jiabing Wang, Carol A. McVean