Ring Nitrogen Is Shared By Two Of The Cyclos Patents (Class 546/94)
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Publication number: 20090117125Abstract: The present disclosure relates to a series of bis(hydroxymethyl) and its bis(carbamate) of 8H-3a-azacyclopenta[a]indene-1-yl and 5,10-dihydropyrrolo-[1,2-b]isoquinolines derivatives (Formula I-Formula IV) as DNA di-alkylating agents. The preliminary antitumor studies indicated that compounds disclosed herein could exhibit potent cytotoxicity in vitro and antitumor therapeutic efficacy in human tumor xenografts and could have little or no cross-resistance to either Taxol or Vinblastine. The results demonstrated that compounds disclosed herein possess potent antitumor therapeutic efficacy and are expected to have potential for clinical applications.Type: ApplicationFiled: November 7, 2008Publication date: May 7, 2009Inventors: Tsann-Long Su, Ting-Chao Chou
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Publication number: 20090117040Abstract: The present invention relates to pharmaceutical and diagnostic compositions as well as to the use of the active substances contained therein for preparing a pharmaceutical or a diagnostic composition for the treatment or diagnosis of neurodegenerative disorders or amyloid diseases.Type: ApplicationFiled: February 11, 2005Publication date: May 7, 2009Applicant: Max-Delbrug-Centrum Fur Molekulare MedizinInventors: Erich Wanker, Sabine Engemann, Susanne Rautenberg, Annett Boeddrich, Phoebe Markovic, Dagmar Ehrnhofer, Martin Herbst, Jacqueline Walther
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Publication number: 20090102371Abstract: To provide a high-performance organic light emitting device and a novel compound possessed by the device. Provided are a novel fluoranthene derivative and an organic light emitting compound having the derivative.Type: ApplicationFiled: April 24, 2007Publication date: April 23, 2009Applicant: CANON KABUSHIKI KAISHAInventors: Masashi Hashimoto, Akihito Saitoh, Naoki Yamada, Satoshi Igawa, Jun Kamatani, Takao Takiguchi, Shinjiro Okada
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Publication number: 20090042227Abstract: Amino(oligo)thiophene dyes useful for studying the electrophysiology of organelles, cells, and tissues are described. Compared to previously known dyes, the amino(oligo)thiophene dyes exhibit improved (faster) response to membrane potential changes, as well as the ability to be excited by 1064 nanometer femtosecond pulses. Methods of preparing the amino(oligo)thiophene dyes are also described.Type: ApplicationFiled: July 30, 2008Publication date: February 12, 2009Inventors: Leslie M. Loew, Ping Yan
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Publication number: 20090030207Abstract: The present invention provides polymorphic forms of dolasetron base and methods for their use and preparation.Type: ApplicationFiled: July 21, 2008Publication date: January 29, 2009Inventors: Janos Hajko, Tivadar Tamas, Adrienne Kovacsne-Mezei, Piroska Kovacs
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Publication number: 20090023739Abstract: This invention provides novel caspase inhibitors of formula I: wherein R1 is hydrogen, CHN2, R, or —CH2Y; R is an aliphatic group, an aryl group, an aralkyl group, a heterocyclyl group, or a heterocyclylalkyl group; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; X2—X1 is N(R3)—C(R3), C(R3)2—C(R3), C(R3)2—N, N?C, C(R3)?C, C(?O)—N, or C(?O)—C(R3); each R3 is independently selected from hydrogen or C1-6 aliphatic; Ring C is a fused aryl ring; n is 0, 1 or 2; and each methylene carbon in Ring A is optionally and independently substituted by ?O, or one or more halogen, C1-4 alkyl, or C1-4 alkoxy. The compounds are useful for treating caspase-mediated diseases.Type: ApplicationFiled: July 1, 2008Publication date: January 22, 2009Applicant: Vertex Pharmaceuticals, IncorporatedInventors: Jean-Damien Charrier, Guy Brenchley
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Patent number: 7462628Abstract: Preventives/remedies for voiding disturbance containing a compound having both of an acetylcholinesterase inhibitory action and an ?1 antagonistic action which exhibits an excellent effect of improving the urinary function of the bladder (i.e., effects of improving urine flow rate and voiding efficiency) without affecting the urinary pressure or the blood pressure.Type: GrantFiled: January 18, 2006Date of Patent: December 9, 2008Assignee: Takeda Pharmaceutical Company LimitedInventors: Yuji Ishihara, Yuji Ishichi, Takayuki Doi, Hiroshi Nagabukuro, Naoyuki Kanzaki, Motoki Ikeuchi
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Publication number: 20080280892Abstract: Tricyclic nitrogen containing compounds and their use as antibacterials.Type: ApplicationFiled: October 17, 2006Publication date: November 13, 2008Inventors: Nathalie Cailleau, David Thomas Davies, Joel Michael Esken, Alan Joseph Hennessy, Senthil Kumar Kusalakumari Sukumar, Roger Edward Markwell, Timothy James Miles, Neil David Pearson
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Publication number: 20080275241Abstract: The present disclosure relates to a process for the preparation of endo-hexahydro-8-(3-indolylcarbonyloxy)-2,6-methano-2H-quinolizin-3(4H)-one or Dolasetron base. It also discloses a process for the preparation of endo-hexahydro-8-(3-indolylcarbonyloxy)-2,6-methano-2H-quinolizin-3(4H)-one mesylate or Dolasetron mesylate. Further, the present disclosure relates to a process for producing Form I of Dolasetron base, and to the novel crystalline polymorphs, Form II, III, IV and V of Dolasetron base and industrial processes for producing them.Type: ApplicationFiled: December 22, 2006Publication date: November 6, 2008Inventors: Venkatasubramanian Radhakrishnan Tarur, Dhananjay Govind Sathe, Nandu Baban Bhise, Kamlesh Digambar Sawant, Tushar Anil Naik, Neeraj Srivastav, Raviraj Bhatu Deore
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Publication number: 20080262023Abstract: The invention relates to compounds that are substituted aminomethyl azaadamantane derivatives, compositions comprising such compounds, and methods of using such compounds and compositions.Type: ApplicationFiled: March 20, 2008Publication date: October 23, 2008Applicant: Abbott LaboratoriesInventors: Lei Shi, Marc J.C. Scanio, William H. Bunnelle
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Publication number: 20080255179Abstract: The invention relates to compounds that are acetamide and carboxamide derivatives of azaadamantane, compositions comprising such compounds, and methods of using such compounds and compositions.Type: ApplicationFiled: March 20, 2008Publication date: October 16, 2008Applicant: ABBOTT LABORATORIESInventors: Marc J.C. Scanio, Lei Shi, William H. Bunnelle, Michael R. Schrimpf
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Publication number: 20080255180Abstract: The invention relates to compounds that are 4-substituted azaadamantane derivatives, compositions comprising such compounds, and methods of using such compounds and compositions.Type: ApplicationFiled: March 20, 2008Publication date: October 16, 2008Applicant: ABBOTT LABORATORIESInventor: William H. Bunnelle
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Publication number: 20080234311Abstract: The present invention provides a method for the detection and quantification of A?1-40 produced in native cell types and tissues. Also provided are assays and kits to determine the effect of compounds on the production of amyloid ? peptides.Type: ApplicationFiled: November 19, 2007Publication date: September 25, 2008Inventors: Jinhe Li, Murali Gopalakrishnan
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Publication number: 20080221090Abstract: The invention encompasses compounds of Formula I as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.Type: ApplicationFiled: March 3, 2008Publication date: September 11, 2008Inventors: Kap-Sun Yeung, John F. Kadow
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Publication number: 20080194824Abstract: The present invention relates to a method for obtaining Dolasetron that comprises: a) Esterification of the alcohol of formula (IV) with indole-3-carboxylic acid (compound (III)) or a reactive derivative thereof, to give a compound of formula (V), followed by step b) which includes Dieckmann reaction of the intermediate (V), by reaction with a strong organic or inorganic base, to give the intermediate (VI), and step c) which comprises dealcoxycarbonylation of the intermediate (VI) to give Dolasetron base and, if desired, a pharmaceutically acceptable salt thereof, hydrates or solvates of the base of said salt. The invention also relates to the intermediates (V) and (VI), and methods for obtaining them. With the method of the present invention Dolasetron is obtained at industrial scale with good yields, with decreased use of reactants and solvents, while said method is also of greater atomic efficiency.Type: ApplicationFiled: June 26, 2006Publication date: August 14, 2008Applicant: INKE, S.A.Inventor: Juan Antonio Perez Andres
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Publication number: 20080169453Abstract: According to the present invention, there is provided a near infrared ray absorbing material comprising at least a first compound having a spectral absorption maximum wavelength of 470 nm or less in a range of 270 to 1600 nm in solution, and a second compound represented by the following formula (II-1) or (II-2). where in the formulas, R201, R202, R211, R212, R221, and R222 each represent, independently, a hydrogen atom, an aliphatic group, an aromatic group, or a heterocyclic group linked via a carbon atom; Z201 and Z202 represent a nonmetal atomic group necessary for forming a nitrogen-containing heterocycle; R213 to R216 and R223 to R226 represent a hydrogen atom or a substituent.Type: ApplicationFiled: August 16, 2007Publication date: July 17, 2008Applicant: FUJIFILM CORPORATIONInventors: Keizo Kimura, Katsuyoshi Yamakawa, Osamu Uchida
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Publication number: 20080161338Abstract: The invention relates to novel pyrrolodihydroisoquinoline derivatives, which are efficacious inhibitors of PDE10.Type: ApplicationFiled: January 11, 2006Publication date: July 3, 2008Applicant: ALTANA PHARMA AGInventors: Matthias Vennemann, Thomas Bar, Jurgen Braunger, Paola Ciapetti, Jean-Marie Contreras, Camille George Wermuth
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Patent number: 7320849Abstract: Improved organophotoreceptor comprises an electrically conductive substrate and a photoconductive element on the electrically conductive substrate, the photoconductive element comprising: (a) a charge transport material having the formula where Y1 and Y2 are, each independently, an arylamine group; R1 and R2 comprise, each independently, H, an alkyl group, an alkenyl group, a heterocyclic group, or an aromatic group; X1 and X2, each independently, are bridging groups; E1 and E2 are, each independently, an epoxy group; and Z is a linking group comprising an alkyl group, an alkenyl group, a heterocyclic group, or an aromatic group; and (b) a charge generating compound. The charge transport materials can be crosslinked to a polymeric bind, either directly or through a crosslinking agent. Corresponding electrophotographic apparatuses and imaging methods are described.Type: GrantFiled: December 31, 2003Date of Patent: January 22, 2008Assignee: Samsung Electronics Co., Ltd.Inventors: Nusrallah Jubran, Zbigniew Tokarski, Vytautas Getautis, Tadas Malinauskas, Vygintas Jankauskas, Valentas Gaidelis
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Patent number: 7247642Abstract: The present invention relates to optically pure S-(?)-benzoquinolizine carboxylic acids, their derivatives, salts, pseudopolymorphs, polymorphs and hydrates thereof, substantially free of their R-(+)-isomers, to processes for preparation of the optically pure S-(?)-benzoquinolizine carboxylic acids, their derivatives, salts, pseudopolymorphs, polymorphs and hydrates thereof substantially free of their R-(+)-isomers, and to pharmaceutical compositions comprising the S(?)-benzoquinolizine carboxylic acids, their derivatives, salts, pseudopolymorphs, polymorphs and hydrates thereof.Type: GrantFiled: May 8, 2000Date of Patent: July 24, 2007Assignee: Wockhardt LimitedInventors: Mahesh Vithalbhai Patel, Shivkumar Agarwal, Sreenivas Kandepu, Nitin Shetty, Dilip Jatashankar Upadhyay, Nishith Chandra Chaturvedi, Abraham Thomas, Noel John De Souza, Habil Fakhruddin Khorakiwala
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Patent number: 7217465Abstract: A light-emitting compound that can be easily applied to vacuum vapor deposition and exhibit long wavelength light is disclosed. Further, a light-emitting element without inferior luminescence properties due to the carbonization of a light-emitting compound during vapor deposition; and a light-emitting device that is composed of the light-emitting elements are also disclosed. A pyran derivative is represented by the following general formula 1: wherein R1 is a hydrogen element or an alkoxy group.Type: GrantFiled: October 19, 2004Date of Patent: May 15, 2007Assignee: Semicondutor Energy Laboratory Co., Ltd.Inventors: Sachiko Yamagata, Hiroko Abe, Nobuharu Ohsawa, Ryoji Nomura, Satoshi Seo
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Patent number: 7164023Abstract: The invention relates to crystalline S-(?)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid L-arginine salt tetrahydrate, a process for its preparation and pharmaceutical formulations incorporating it as the active ingredient for use in treating microbial infections.Type: GrantFiled: December 31, 2003Date of Patent: January 16, 2007Assignee: Wockhardt LimitedInventors: Prasad K. Deshpande, Vijaya N. Desai, Ravindra D. Yeole, Shrikant V. Gupte, Mahesh V. Patel, Noel J. de Souza
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Patent number: 7144913Abstract: Dihydropyrroloindoles and tetrahydropyridoindoles are prostaglandin receptor antagonists useful for the treatment of prostaglandin-mediated diseases such as allergic rhinitis, nasal congestion and asthma.Type: GrantFiled: May 22, 2002Date of Patent: December 5, 2006Assignee: Merck Frosst Canada & Co.Inventors: Zhaoyin Wang, Christian Beaulieu, Claude Dufresne, Daniel Guay, Yves LeBlanc
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Patent number: 7135480Abstract: The present invention is directed to substituted 1-benzoyl-3-cyano-pyrrolo[1,2-?]quinolines and analogs thereof, represented by the general Formula I: wherein R1–R8, L, Q, dash line and Ar are defined herein. The present invention also relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.Type: GrantFiled: December 12, 2003Date of Patent: November 14, 2006Assignee: Cytovia, Inc.Inventors: Sui Xiong Cai, John A Drewe, Sungchun Jiang, Shailaja Kasibhatla, Jared Daniel Kuemmerle, Nilantha Sudath Sirisoma, Han-Zhong Zhang
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Patent number: 7132541Abstract: The invention relates to the new arginine salt forms of RS-(±)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid, S-(?)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid, R-(+)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid, a process for their preparation and pharmaceutical formulations which comprise those arginine salt forms as the active ingredient for its use in treating microbial infections.Type: GrantFiled: September 25, 2003Date of Patent: November 7, 2006Assignee: Wockhardt LimitedInventors: Noel J. de Souza, Prasad K Deshpande, Milind C. Shukla, Siddiqui M Jaweed Mukarram, Dilip Ganesh Kulkarni, Ansari Azizur Rahman, Ravindra D Yeole, Mahesh V Patel, Shrikant V Gupte
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Patent number: 7122555Abstract: The present invention provides compounds of formula (I) wherein R1, R2, R3 and R4 are as indicated in the description, or a pharmaceutically acceptable salt thereof. The compounds are useful for the treatment of diseases which are associated with DPP-IV, such as diabetes, particularly non-insulin dependent diabetes mellitus, and impaired glucose tolerance.Type: GrantFiled: June 17, 2004Date of Patent: October 17, 2006Assignee: Hoffmann-la Roche Inc.Inventors: Markus Boehringer, Bernd Kuhn, Patrizio Mattei, Robert Narquizian
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Patent number: 7091352Abstract: Compounds of the formula (I) below, or pharmacologically acceptable salts, esters or other derivatives thereof: wherein A is furan, thiophene, pyrazole, imidazole, isoxazole or isothiazole; R1 is a substituted or unsubstituted aryl or a substituted or unsubstituted heteroaryl; R2 is a substituted or unsubstituted heteroaryl; and R3 is a bicyclic amino group; provided that the substituents R1 and R2 are bonded to the two atoms of the cyclic group A which are adjacent to the atom of the cyclic group A to which the substituent R2 is bonded. The compounds inhibit the production of inflammatory cytokines.Type: GrantFiled: July 22, 2003Date of Patent: August 15, 2006Assignee: Sankyo Company, LimitedInventors: Tomio Kimura, Akira Nakao
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Patent number: 7081531Abstract: Compounds having the formula (I), Ar—(F)-(E)-(CR3R4)—(CHR5)m-(T)-(Q)-Ar1, are useful as CCR-3 receptor antagonists, wherein T is a bridged heterocyclyl group having one N atom and a bridge of one to two bridgehead carbon atoms; Ar and Ar1 are aryl or heteroaryl; F is alkylene, alkenylene, or a bond; E is —C(?O)N(R10)—, —SO2N(R10)—, —N(R11)C(?O)N(R10)—, —N(R11)SO2N(R10)—, —N(R11)C(?S)N(R10)—, —N(R11)C(?O)—, —N(R11)SO2—, —N(R12)C(?O)CH(R13)—, or CH(R13)C(?O)N(R12)—; Q is —C(?O)— or C1-2alkylene; and R3, R4, R5, R9, R10, R11, R12, and R13 are defined as set forth in the specification.Type: GrantFiled: February 26, 2004Date of Patent: July 25, 2006Assignee: Roche Palo Alto LLCInventor: Leyi Gong
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Patent number: 7029606Abstract: A dihydrofuran-containing nonlinear optical chromophore having a ?-electron donor group conjugated to the dihydrofuran group through a ?-electron conjugated bridge group. The nonlinear optical chromophore is a hyperpolarizable chromophore that can be used as an electro-optic modulator in electro-optic devices.Type: GrantFiled: July 24, 2001Date of Patent: April 18, 2006Assignee: University of WashingtonInventors: Larry R. Dalton, Kwan-Yue Jen, Timothy Londergan, William Brenden Carlson, Gregory Phelan, Diyun Huang, Daniel Casmier, Todd Ewy, Nicholas Buker
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Patent number: 7022729Abstract: Azabicyclic, azatricyclic and azaspirocyclic derivatives of aminocyclohexanes which are systemically-active as NMDA, 5HT3, and nicotinic receptor antagonists, pharmaceutical compositions comprising the same, method of preparation thereof, and method of treating CNS disorders which involve disturbances of glutamatergic, serotoninergic, and nicotinic transmission, treating immunomodulatory disorders, and antimalaria, antitrypanosomal, anti-Borna virus, anti-HSV and anti-Hepatitis C virus activity.Type: GrantFiled: March 21, 2003Date of Patent: April 4, 2006Assignee: Merz Pharma GmbH & Co. KGAAInventors: Christopher Graham Raphael Parsons, Markus Henrich, Wojciech Danysz, Ivars Kalvinsh, Valerjans Kauss, Aigars Jirgensons, Markus Gold, Maksims Vanejevs
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Patent number: 6964833Abstract: Improved organophotoreceptors comprise: (a) a charge transport compound having the formula where n is an integer from 0 to 1; X is an (N,N-disubstituted)arylamine group; Ar is an aryl group or a heterocyclic group; A is a first linking group with the formula —(CH2)p— which can be branched or linear, where p is an integer from 3 to 20 inclusive; and B is a second linking group having the formula -Q-Z-Q?-, where Q and Q? are, independently, O, S, or NR1; wherein when Q or Q? is NR1 or Q=O and Q?=S, Z comprises an aryl group, and wherein when Q=Q?=S or Q=Q?=O, Z comprises a multi-ring conjugated group or Y—W—Y?, where the groups R1, Y, W, and Y? are defined in the specification; (b) a charge generating compound; and (c) an electrically conductive substrate over which said charge transport compound and said charge generating compound are located.Type: GrantFiled: May 7, 2003Date of Patent: November 15, 2005Assignee: Samsung Electronics Co., Ltd.Inventors: Zbigniew Tokarski, Nusrallah Jubran, Vytautas Getautis, Edmundas Montrimas, Maryte Daskeviciene, Valentas Gaidelis, Vygintas Jankauskas
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Patent number: 6930114Abstract: The present invention relates to pyrrolo[2.1-a]dihydroisoquinolines which are inhibitors of phosphodiesterase 10a and can be used for combating cancer.Type: GrantFiled: December 4, 2001Date of Patent: August 16, 2005Assignee: Bayer Pharmaceuticals CorporationInventors: Maria Theresia Niewöhner, Marcus Bauser, Jens-Kerim Ergüden, Dietmar Flubacher, Paul Naab, Thorsten-Oliver Repp, Jürgen Stoltefuss, Nils Burkhardt, Andrea Sewing, Michael Schauer, Karl-Heinz Schlemmer, Olaf Weber, Stephen J. Boyer, Mark Miglarese, Ulrich Niewöhner
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Patent number: 6887868Abstract: The present invention provides compounds of Formula (I): wherein: R1, R2, R3, R4, R5, R6 R7, R8, n, m, and X have any of the values defined in the specification, as well as pharmaceutical compositions comprising the compounds. The invention also provides therapeutic methods as well as processes and intermediates useful for preparing compounds of Formula (I). The compounds are 5-HT ligands and are useful for treating diseases wherein modulation of 5-HT activity is desired.Type: GrantFiled: September 19, 2002Date of Patent: May 3, 2005Assignee: Pharmacia & Upjohn CompanyInventor: Jian-Min Fu
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Patent number: 6881842Abstract: A process for easily and industrially advantageously producing both a tricyclic fused heterocyclic derivative having acetylcholinesterase inhibitory activity and an intermediate for the derivative. The process for producing the target compounds comprises the following reaction.Type: GrantFiled: September 20, 2001Date of Patent: April 19, 2005Assignee: Takeda Chemical Industries, Ltd.Inventors: Tadao Kawarasaki, Hideo Hashimoto, Kiminori Tomimatsu
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Patent number: 6878713Abstract: This invention relates to new generation triple-targeting, chiral, broad-spectrum antimicrobial 7-substituted piperidino-quinolone carboxylic acid derivatives, to their optical isomers, diastereomers or enantiomers, as well as pharmaceutically acceptable salts, hydrates, prodrugs, polymorphs and pseudopolymorphs thereof, to their preparation, to their compositions and to their use.Type: GrantFiled: December 12, 2002Date of Patent: April 12, 2005Assignee: Wockhardt LimitedInventors: Noel John De Souza, Mahesh Vithalbhai Patel, Prasad Keshav Deshpande, Shiv Kumar Agarwal, Kandepu Sreenivas, Sheela Chandrasekharan Nair, Yati Chugh, Milind Chintaman Shukla
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Patent number: 6867198Abstract: The present invention provides selective kinase inhibitors of formula (I)Type: GrantFiled: December 18, 2000Date of Patent: March 15, 2005Assignee: Eli Lilly and CompanyInventors: Rima Salim Al-Awar, Kyle Andrew Hecker, James Edward Ray, Jianping Huang, Sajan Joseph, Tiechao Li, Michael Paal, Radhakrishnan Rathnachalam, Chuan Shih, Philip Parker Waid, Xun Zhou, Guoxin Zhu
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Patent number: 6858613Abstract: The invention provides compounds of Formula I: These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals to treat conditions or diseases in which ?7 is known to be involved.Type: GrantFiled: February 14, 2003Date of Patent: February 22, 2005Assignee: Pfizer Inc.Inventors: Bruce N. Rogers, David W. Piotrowski, Daniel Patrick Walker, Eric Jon Jacobsen, Brad A. Acker, Donn G. Wishka, Vincent E. Groppi, Jr.
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Patent number: 6844089Abstract: The invention relates to an electroluminescent device, in which the luminescent layer contains a luminescent compound and a compound of the general formula I as doping agent, wherein B is an unsaturated carbocyclic or heterocyclic 4-8-link ring, which can also contain an alicyclic bridge, the rings D and E are five- or six-link rings, which each can contain one more hetero-atom N, O and S, the radicals R are one or more substituents H or straight-chain or branched C1-C6-alkyl, X and Y are carbon or nitrogen, R1; R2 and R9 are H or straight-chain or branched C1-C6-alkyl, R3 and R9 are hydrogen, straight-chain or branched C1-C6-alkyl, hydroxy, —OR16, —COOR16, N,N-dialkylamino, acetylamino or halogen, wherein R16 is hydrogen, or straight-chain or branched C1-C6-alkyl, R1 and R2 or R2 and R3 and/or R9 and R9 together can form an alicyclic, heterocyclic or aromatic ring, and A1 and A2, which can be the same or different, are cyan, nitro or —COOR16. The compounds I are partly new.Type: GrantFiled: May 10, 2002Date of Patent: January 18, 2005Assignee: Sensient Imaging Technologies GmbHInventors: Andreas Richter, Dietmar Keil, Gerhard Diener
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Publication number: 20040259903Abstract: The present invention provides compounds of formula (I) 1Type: ApplicationFiled: June 17, 2004Publication date: December 23, 2004Inventors: Markus Boehringer, Bernd Kuhn, Patrizio Mattei, Robert Narquizian
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Patent number: 6833202Abstract: Organic electroluminescence devices are described, each of which comprises an anode, a cathode, a luminescent layer, at least one hole-transporting layer disposed between the anode and the luminescent layer, at least one electron-transporting layer disposed between the cathode and the luminescent layer, and a substrate present on either the anode or cathode. The luminescent layer in the devices uses as red-emitting materials, salicylaldiminato Schiff bases or their metal complexes based on diaminomaleonitrile and salicylaldehyde derivatives. These organic electroluminescence devices exhibit excellent color chromaticity co-ordinates and good efficiency.Type: GrantFiled: March 13, 2003Date of Patent: December 21, 2004Assignee: City University of Hong KongInventors: Shuit-Tong Lee, Chun-Sing Lee, Peng-Fei Wang, Zhi-Yuan Xie
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Publication number: 20040214850Abstract: Disclosed is a compound represented by Structural Formula (I): 1Type: ApplicationFiled: May 20, 2004Publication date: October 28, 2004Applicant: Synta Pharmaceuticals Corp.Inventors: Keizo Kova, Lijun Sun, Mitsunori Ono, Weiwen Ying, Hao Li
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Publication number: 20040180234Abstract: Organic electroluminescence devices are described, each of which comprises an anode, a cathode, a luminescent layer, at least one hole-transporting layer disposed between the anode and the luminescent layer, at least one electron-transporting layer disposed between the cathode and the luminescent layer, and a substrate present on either the anode or cathode. The luminescent layer in the devices uses as red-emitting materials, salicylaldiminato Schiff bases or their metal complexes based on diaminomaleonitrile and salicylaldehyde derivatives. These organic electroluminescence devices exhibit excellent color chromaticity co-ordinates and good efficiency.Type: ApplicationFiled: March 13, 2003Publication date: September 16, 2004Inventors: Shuit-Tong Lee, Chun-Sing Lee, Peng-Fei Wang, Zhi-Yuan Xie
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Publication number: 20040162279Abstract: The invention includes tetrahydroquinoline and related compounds of formula I, and pharmaceutical compositions thereof, that exhibit useful antibacterial activity against a wide range of human and veterinary pathogens.Type: ApplicationFiled: October 2, 2003Publication date: August 19, 2004Inventors: Michael Robert Barbachyn, J. Craig Ruble, Arthur Glenn Romero, Lisa Marie Thomasco, Alexander Ross Hurd, John Raymond Palmer, Peter Laurence Toogood, Dennis Joseph McNamara, Debra Ann Sherry, Paul Joseph Dobrowolski
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Publication number: 20040138249Abstract: The present invention relates to pyrrolo[2.1-a]dihydroisoquinolines which are inhibitors of phosphodiesterase 10a and can be used for combating cancer.Type: ApplicationFiled: February 9, 2004Publication date: July 15, 2004Inventors: Ulrich Niewohner, Maria Theresia Niewohner, Marcus Bauser, Jens-Kerim Erguden, Dietmar Flubacher, Paul Nabb, Thorsten-Oliver Repp, Jurgen Stoltefuss, Nils Burkhardt, Andrea Sewing, Michael Schauer, Karl-Heinz Schlemmer, Olaf Weber, Stephen J. Boyer, Mark Miglarese
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Publication number: 20040131849Abstract: A polymerizable resin material for making a plastic lens includes bisphenol A ethoxylate (1 to 4) dimethacrylate and benzylmethacrylate, and, optionally, one or more stabilizing monomers, preferably selected from trimethylolpropane trimethacrylate, isobornyl methacrylate, ethoxylate nonyl phenol acrylate, ethyoxylate nonyl phenol, and/or 2-phenoxyethyl methacrylate esters. The polymerizable resin material is cured when exposed to heat or visible and/or UV light for a period of about two minutes or less.Type: ApplicationFiled: December 19, 2000Publication date: July 8, 2004Inventor: Duane L. Wires
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Patent number: 6753333Abstract: The invention relates to the new arginine salt forms of S-(−)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid, a process for their preparation and pharmaceutical formulations which comprise those arginine salt forms as the active ingredient for its use in treating antimicrobial infections.Type: GrantFiled: November 22, 2002Date of Patent: June 22, 2004Assignee: Wockhardt LimitedInventors: Noel J. De Souza, Shivkumar Agarwal, Mahesh V. Patel, Satish B. Bhawsar, Rupinder K. Beri, Ravindra D. Yeole, Nitin Shetty
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Patent number: 6750224Abstract: The present invention relates to optically pure S-(−)-benzoquinolizine carboxylic acids, their derivatives, salts, pseudopolymorphs, polymorphs and hydrates thereof, substantially free of their R-(+)-isomers, to processes for preparation of the optically pure S-(−)-benzoquinolizine carboxylic acids, their derivatives, salts, pseudopolymorphs, polymorphs and hydrates thereof substantially free of their R-(+)-isomers, and to pharmaceutical compositions comprising the S(−)-benzoquinolizine carboxylic acids, their derivatives, salts, pseudopolymorphs, polymorphs and hydrates thereof.Type: GrantFiled: August 17, 2000Date of Patent: June 15, 2004Assignee: Wockhardt LimitedInventors: Mahesh Vithalbhai Patel, Shivkumar Agarwal, Sreenivas Kandepu, Nitin Shetty, Dilip Upadhyay, Nishith Chaturvedi, Abraham Thomas, Noel John De Souza, Habil Fakhruddin Khorakiwala
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Patent number: 6727261Abstract: The present invention provides compounds of formula (I) wherein R1, R2, R3, R4, R5 and R6 are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with DPP-IV, such as diabetes, particularly non-insulin dependent diabetes mellitus, and impaired glucose tolerance.Type: GrantFiled: December 17, 2002Date of Patent: April 27, 2004Assignee: Hoffman-La Roche Inc.Inventors: Luca Claudio Gobbi, Thomas Luebbers, Patrizio Mattei, Robert Narquizian, Pierre Charles Wyss
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Patent number: 6706880Abstract: The invention relates to novel compounds which show high affinity for cocaine receptors in the brain, particularly dopamine and serotonin transporter sites. The compounds may be used as imaging or pharmaceutical agents, in the diagnosis and treatment of drug addiction, depression, anorexia and neurodegenerative diseases or in determining the doses of therapeutic agents that occupy significant numbers of receptors.Type: GrantFiled: September 20, 2001Date of Patent: March 16, 2004Assignee: Research Triangle InstituteInventors: Frank I. Carroll, Michael J. Kuhar, John W. Boja, Anita H. Lewin, Philip Abraham
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Patent number: 6696462Abstract: A compound of formula 1 wherein: X- is an anion with a single negative charge; A and B, which are identical or different, are each —O—, —S—, —NH—, —CH2—, —CH═CH—, or —N(C1-C4-alkyl)—; R is hydrogen, hydroxy, —C1-C4-alkyl, —C1-C4-alkyloxy, —C1-C4-alkylene-halogen, —0—C1-C4-alkylene-halogen, —C1-C4-alkylene-OH, —CF3, —CHF2, —C1-C4-alkylene-C1-C4-alkyloxy, —0—COC1-C4-alkyl, —0—COC1-C4-alkylene-halogen, —C1-C4-alkylene-C3-C6-cycloalkyl, —0—COCF3, or halogen; R1 and R2, which are identical or different, are each —C1-C5-alkyl, which is optionally substituted by —C3-C6-cycloalkyl, hydroxy, or halogen, or R1 and R2 together are a —C3-C5-alkylene bridge; R3, R4, R3′, and R4′, which are identical or different, are each hydrogen, C1-C4-alkyl, C1-C4-alkyloxy, hydroxy, —CF3, —CHF2, &mdasType: GrantFiled: January 16, 2003Date of Patent: February 24, 2004Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Christian Eickmeier, Sabine Germeyer, Matthias Grauert, Sabine Pestel, Michael P. Pieper, Georg Speck, Steffen Breitfelder
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Publication number: 20040029879Abstract: The present invention provides a compound of formula I 1Type: ApplicationFiled: July 31, 2003Publication date: February 12, 2004Inventors: David John Anderson, Thomas J. Beauchamp, Gordon L. Bundy, Fred L. Ciske, John R. Farrell, David R. Graber, Michael J. Genin, Thomas M. Judge, Malcolm Wilson Moon, Mark E. Schnute, Joseph Walter Strohbach, Suvit Thaisrivongs, Atli Thorarensen, Steven Ronald Turner, Valerie A. Vaillancourt, Allison J. Wolf