Polycyclo Heterocyclic Ring System Containing Ring Nitrogen Patents (Class 548/181)
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Patent number: 7569688Abstract: Provided is a pharmaceutical composition containing a propane-1,3-dione derivative as the active ingredient, particularly a GnRH receptor antagonist. Also, provided is a propane-1,3-dione derivative having a GnRH antagonistic effect.Type: GrantFiled: June 20, 2005Date of Patent: August 4, 2009Assignee: Astellas Pharma Inc.Inventors: Masaaki Hirano, Eiji Kawaminami, Akira Toyoshima, Hiroyuki Moritomo, Norio Seki, Ryutaro Wakayama, Minoru Okada, Toshiyuki Kusayama
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Publication number: 20090192204Abstract: The present invention relates to the use of N-(2-thiazolyl)-amide derivatives of formula (I) for the treatment and/or prophylaxis of a disease in which glycogen synthase kinase 3 (GSK-3) is involved, especially neurodegenerative diseases, such as Alzheimer's disease, or non-insulin dependent diabetes mellitus.Type: ApplicationFiled: April 27, 2007Publication date: July 30, 2009Applicant: NOSCIRA, S.A.Inventors: Ana Martinez Gil, Ana Castro Morera, Miguel Medina Padilla, Ester Martin Aparicio, Mercedes Alonso Cascon, Ana Fuertes Huerta, Maria Luisa Navarro Rico, Maria Jose Perez Puerto, Maria Del Monte Millan
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Patent number: 7560568Abstract: The present invention provides compounds of formula (I): wherein all variables are as defined herein, pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents.Type: GrantFiled: December 2, 2004Date of Patent: July 14, 2009Assignee: SmithKline Beecham CorporationInventor: Kyle Allen Emmitte
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Publication number: 20090176822Abstract: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, Q, X1, X2, Y, R1, R2, R3, R4, R4?, R5, R6 and R6? are as described herein.Type: ApplicationFiled: April 17, 2008Publication date: July 9, 2009Applicant: Genentech, Inc.Inventors: Frederick Cohen, Vickie Hsiao-Wei Tsui, Cuong Ly, John A. Flygare
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Publication number: 20090143353Abstract: A 1,6-?-glucan synthetase inhibitor is provided, having potent growth inhibition and having excellent safety. A compound is provided, capable of expressing in a wide spectral range and specifically or selectively, an antifungal effect based on its functional mechanism of 1,6-?-glucan synthesis inhibition. Also provided is a drug, especially an antifungal that contains the compound, its salt or their hydrate.Type: ApplicationFiled: August 16, 2006Publication date: June 4, 2009Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Katsuhiro Kawakami, Kazuo Kanai, Takao Horiuchi, Hiroshi Takeshita, Syozo Kobayashi, Yuichi Sugimoto, Issei Achiwa, Junichi Kuroyanagi
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Patent number: 7541354Abstract: Bicyclo-pyrazole compounds of formula (I), as herein defined, are useful for treating diseases linked to disregulated protein kinases.Type: GrantFiled: July 25, 2001Date of Patent: June 2, 2009Assignee: Pfizer Italia S.r.l.Inventors: Daniele Fancelli, Valeria Pittala, Mario Varasi
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Publication number: 20090137644Abstract: This invention describes compounds and pharmaceutical compositions useful as inhibitors of ubiquitination. The compounds and compositions of the invention are useful as inhibitors of the biochemical pathways of organisms in which ubiquitination is involved. In particular, the compounds and compositions are useful for treating diseases caused by viruses such as poxviruses and retroviruses. The invention further provides for methods of treating smallpox, Herpes virus and HIV infection in patients using the compounds and compositions of the invention.Type: ApplicationFiled: October 28, 2004Publication date: May 28, 2009Applicant: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Usha Ramesh, Sarkiz D. Issakani, Gary Charles Look
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Publication number: 20090131401Abstract: Substituted benzoimidazole compounds useful as anti-infectives that decrease resistance, virulence, or growth of microbes are provided. Methods of making and using substituted benzoimidazole compounds, as well as pharmaceutical preparations thereof, in, e.g., reducing antibiotic resistance and inhibiting biofilms.Type: ApplicationFiled: February 12, 2008Publication date: May 21, 2009Applicant: Paratek Pharmaceuticals, Inc.Inventors: Stuart B. Levy, Michael N. Alekshun, Brent L. Podlogar, Kwasi Ohemeng, Atul K. Verma, Tadeusz Warchol, Beena Bhatia, Todd Bowser, Mark Grier
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Publication number: 20090105318Abstract: The present invention is directed to amidoethylthioether compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.Type: ApplicationFiled: March 27, 2007Publication date: April 23, 2009Inventors: Paul J. Coleman, John D. Schreier
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Patent number: 7511059Abstract: The invention relates to thiazolidinones of general formula (I) their production and use as inhibitors of polo-like kinases (Plk) for treating various diseases.Type: GrantFiled: February 2, 2006Date of Patent: March 31, 2009Assignee: Schering AgInventors: Volker Schulze, Knut Eis, Lars Wortmann, Dirk Kosemund, Olaf Prien, Gerhard Siemeister, Holger Hess-Stumpp, Uwe Eberspaecher, Damian O Arnaiz
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Patent number: 7504513Abstract: The invention is directed to compounds of formula (1) and pharmaceutically acceptable salts thereof, methods for the preparation thereof, and methods of use thereof.Type: GrantFiled: February 7, 2007Date of Patent: March 17, 2009Assignee: Hoffman-La Roche Inc.Inventors: John Frederick Boylan, Jianping Cai, Nader Fotouhi, Paul Gillespie, Robert Alan Goodnow, Jr., Kang Le, Christophe Michoud
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Publication number: 20090060874Abstract: The present invention discloses compounds of formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with said compounds.Type: ApplicationFiled: September 5, 2008Publication date: March 5, 2009Inventors: Yao-Ling QIU, Ce WANG, Lu YING, Yat Sun OR
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Publication number: 20090012117Abstract: Bicyclic derivatives having formula (I) and a composition thereof are useful as ion channel antagonists:Type: ApplicationFiled: May 8, 2006Publication date: January 8, 2009Inventors: Aarti S. Kawatkar, Tara M. Whitney, Timothy D. Neubert, Nicole Zimmermann, Andreas Termin, Esther Martinborough
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Publication number: 20090005344Abstract: Imidazole and benzimidazole boronic acid compounds, analogs thereof, and pharmaceutical formulations are described, along with methods of use thereof for inhibiting inflammatory cytokines such as tumor necrosis factor alpha (TNF-?) in a subject in need thereof.Type: ApplicationFiled: October 27, 2005Publication date: January 1, 2009Applicant: NKUADA, LLCInventors: James F. Burns, Leonardo A. Cabana, Glenn C. Collupy, John R. Didsbury, Tatyana A. Dyakonov, Simon N. Haydar, Michael L. Jones, Francine F. Li, Christopher J. Markworth, Jessymol Mathew, Frank J. Schoenen, David S. Van Vliet, David Middlemiss
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Patent number: 7470792Abstract: The present invention provides a synthesis for the preparation of epothilone derivatives of formula 9 wherein R1 is methyl, and R2 is an unsubstituted or substituted aryl; an unsubstituted or substituted heteroaryl; or an unsubstituted or substituted heterocyclic radical fused to a benzene nucleus; and salts thereof, and intermediates for the synthesis of a compound of formula 9.Type: GrantFiled: September 12, 2003Date of Patent: December 30, 2008Assignee: Novartis AGInventors: Guido Koch, Olivier Loiseleur
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Patent number: 7470793Abstract: This invention relates to novel thiazole(bi)cycloalkylcarboxanilides of the formula (I) in which Q and R1 are as defined in the disclosure, to a process for preparing these compounds and to their use for controlling unwanted microorganisms.Type: GrantFiled: October 15, 2003Date of Patent: December 30, 2008Assignee: Bayer CropScience AGInventors: Ralf Dunkel, Heiko Rieck, Hans-Ludwig Elbe, Jörg Nico Greul, Ulrike Wachendorff-Neumann, Karl-Heinz Kuck, Peter Dahmen
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Publication number: 20080293684Abstract: The present invention is directed to compounds which are potentiators of metabotropic glutamate receptors, including the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.Type: ApplicationFiled: July 26, 2005Publication date: November 27, 2008Inventors: Anthony B Pinkerton, Jean-Michel Vernier, Rowena V. Cube, John H. Hutchinson, Dehua Huang, Celine Bonnefous, Steven P. Govak, Theodore Kamenecka
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Publication number: 20080269295Abstract: The present invention relates to substituted thiazoles, to methods for their production, to drugs containing these compounds and to the use of said compounds for producing drugs.Type: ApplicationFiled: June 26, 2008Publication date: October 30, 2008Applicant: Grunenthal GmbHInventors: Michael HAURAND, Klaus SCHIENE, Sven KUHNERT, Melanie REICH
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Patent number: 7439258Abstract: A compound of the formula I: wherein: X is CH or N; Y is O or S; Z is OH, NH2, NMeR3, NHR3; OR3 or 5- or 6-membered heterocycle, having 1 to 4 heteroatoms selected from O, N and S, said heterocycle being optionally substituted with from 1 to 4 substituents; A is N, COR7 or CR5, wherein R5 is H, halogen, or (C1-6) alkyl and R7 is H or (C1-6 alkyl), with the proviso that X and A are not both N; R6 is H, halogen, (C1-6 alkyl) or OR7, wherein R7 is H or (C1-6 alkyl); R1 is selected from the group consisting of 5- or 6-membered heterocycle having 1 to 4 heteroatoms selected from O, N, and S, phenyl, phenyl(C1-3)alkyl, (C2-6)alkenyl, phenyl(C2-6)alkenyl, (C3-6)cycloalkyl, (C1-6)alkyl, CF3, 9- or 10-membered heterobicycle having 1 to 4 heteroatoms selected from O, N and S, wherein said heterocycle, phenyl, phenyl(C2-6)alkenyl and phenyl(C1-3)alkyl), alkenyl, cycloalkyl, (C1-6)alkyl, and heterobicycle are all optionally substituted with from 1 to 4 substituents; R2 is selected from (C1-6)alkyl, (C3-7)cycloalkyl,Type: GrantFiled: May 21, 2004Date of Patent: October 21, 2008Assignee: Boehringer Ingelheim (Canada) LtdInventors: Pierre Louis Beaulieu, Gulrez Fazal, James Gillard, George Kukolj, Volkhard Austel
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Patent number: 7423058Abstract: The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.Type: GrantFiled: December 21, 2006Date of Patent: September 9, 2008Assignee: Schering CorporationInventors: Stephane L. Bogen, Weidong Pan, Sumei Ruan, Kevin X. Chen, Ashok Arasappan, Srikanth Venkatraman, Latha G. Nair, Mousumi Sannigrahi, Frank Bennett, Anil K. Saksena, F. George Njoroge, Viyyoor M. Girijavallabhan
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Publication number: 20080194656Abstract: The present invention relates to a group of benzotriazole derivatives, infra that are potent cannabinoid-CB1 modulators (known as antagonists or inverse agonists), useful in the treatment obesity, psychiatric and neurological disorders, as well as other diseases involving cannabinoid-CB1 neurotransmission (Current Opinion in Drug Discovery & Development 2004 7(4):498-506) the pharmaceutically acceptable acid addition salts and stereoisomeric forms thereof, wherein R1 is hydrogen, halo, trifluoromethyl, C1-4alkyl, C1-4alkyloxy- or C1-4alkyloxycarbonyl; R2 is hydrogen, phenyl, C3-7cycloalkyl or C1-6alkyl optionally substituted with Ar1; R3 is hydrogen, hydroxyl or C1-6alkyl; Ar1 is phenyl or phenyl substituted with up to three halo substituents; and Het represents a monocyclic 5 or 6 membered partially saturated or aromatic heterocycle selected from furanyl, thienyl, pyrrolyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, isoxazolyl, isothiazolyl, oxadiazolyl, triazolyl, thiadiazolyl, pyrimidinyl, pyridType: ApplicationFiled: April 24, 2006Publication date: August 14, 2008Inventors: Monique Jenny Marie Berwaer, Joannes Theodorus Maria Linders, Peter John King, Geert Maria Robert Van Hecke
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Patent number: 7399765Abstract: Compounds of formula (I) Z-Ar1—Ar2??(I) wherein Z is a diazabicyclic amine, Ar1 is a 5- or 6-membered aromatic ring, and Ar2 is selected from the group consisting of an unsubstituted or substituted 5- or 6-membered heteroaryl ring; unsubstituted or substituted bicyclic heteroaryl ring; 3,4-(methylenedioxy)phenyl; carbazolyl; tetrahydrocarbazolyl; naphthyl; and phenyl; wherein the phenyl is substituted with 0, 1, 2, or 3 substituents in the meta- or para-positions. The compounds are useful in treating conditions or disorders prevented by or ameliorated by ?7 nAChR ligands. Also disclosed are pharmaceutical compositions comprising compounds of formula (I) and methods for using such compounds and compositions.Type: GrantFiled: September 16, 2004Date of Patent: July 15, 2008Assignee: Abbott LaboratoriesInventors: William H. Bunnelle, Jianguo Ji, Tao Li, Jennifer M. Pace, Karin R. Tietje, Kathleen H. Mortell, Diana L. Nersesian, Michael R. Schrimpf
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Patent number: 7396838Abstract: A method of treating cancer including administering to a subject in need thereof an effective amount of a compound of the formula 1: wherein R1, R2, R3, R4, and n are as defined herein.Type: GrantFiled: June 6, 2005Date of Patent: July 8, 2008Assignee: National Health Research InstitutesInventors: Chiung-Tong Chen, Shu-Jen Chen, Ming-Chu Hsu, Der-Ren Hwang, Wen-Tai Li, Chu-Chung Lin
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Patent number: 7396833Abstract: The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nAChR), activation of nAChRs, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds for example, indoles, 1H-indazoles, 1,2-benzisoxazoles, and 1,2-benzisothiazoles, which act as ligands for the ?7 nAChR subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.Type: GrantFiled: December 22, 2004Date of Patent: July 8, 2008Assignee: Memory Pharmaceuticals CorporationInventors: Wenge Xie, Brian Herbert, Jianguo Ma, Truc Minh Nguyen, Richard Schumacher, Carla Maria Gauss, Ashok Tehim
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Publication number: 20080153805Abstract: The invention is concerned with novel sulfonamide derivatives of formula (I) wherein R1, R2, R3, X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used as medicaments.Type: ApplicationFiled: December 6, 2007Publication date: June 26, 2008Inventors: Simona M. Ceccarelli, Odile Chomienne, Patrizio Mattei, Ulrike Obst Sander
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Publication number: 20080153816Abstract: Indole compounds corresponding to the formula (I): as defined in the claims, pharmaceutically acceptable addition salts of such compounds, pharmaceutical compositions containing such compounds, the process for their preparation, and their use as pharmacologically active substances, especially in the treatment of hypertriglyceridemia, hyperlipidemia, hypercholesterolemia, diabetes, endothelial dysfunction, cardiovascular disease, inflammatory disease and neurodegeneration.Type: ApplicationFiled: February 28, 2008Publication date: June 26, 2008Applicant: Laboratoires Fournier S.A.Inventors: Jean BINET, Benaissa Boubia, Pierre Dodey, Christiane Legendre, Martine Barth, Olivia Poupardin-Olivier
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Publication number: 20080146594Abstract: Disclosed herein are compounds of Formula (I), (II), and (III) pharmaceutical compositions comprising the same, methods of modulating the activity a thrombopoietin receptor using the same, methods of identifying compounds as thrombopoietin receptor modulators, and methods of treating disease by administering a compound of the invention to a patient in need thereof.Type: ApplicationFiled: November 8, 2007Publication date: June 19, 2008Applicant: Ligand Pharmaceutical, Inc.Inventors: Jyun-Hung Chen, E. Adam Kallel, Thomas Lau, Matthew H. McNeill, Todd A. Miller, Bao N. Nguyen, Richard J. Penuliar, Dean P. Phillips, Daniel A. Ruppar, Lin Zhi, Jackline E. Dalgard
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Publication number: 20080119456Abstract: Compounds of formula (I) are useful for the treatment of disease responsive to modulation of CRTH2 receptor activity, such as asthma, rhinitis, allergic airway syndrome, and allergic rhinobronchitis; wherein X1 is —S—, —O—, —N?N—. —NR7—, —CR7?CR8—, —CR7?N—, wherein R7 and R8 are independently hydrogen or C1-C3 alkyl; A is a carboxyl group —COOH, or a carboxyl bioisostere; rings Ar2 and Ar3 each independently represent a phenyl or 5- or 6-membered monocyclic heteroaryl ring, or a bicyclic ring system consisting of a 5- or 6-membered carbocyclic or heterocyclic ring which is benz-fused or fused to a 5- or 6-membered monocyclic heteroaryl ring, said ring or ring system being optionally substituted; ring B is as defined for Ar2 and Ar3, or an optionally substituted N-pyrrolidinyl, N-piperidinyl or N-azepinyl ring; s is 0 or 1; L1, L2 and L4 are linker radicals as defined in the description; Q1 and Q2 represent substituents as defined in the description.Type: ApplicationFiled: May 30, 2005Publication date: May 22, 2008Inventors: Trond Ulven, Thomas Frimurer, Oystein Rist, Evi Kostenis, Thomas Hogberg, Jean-Marie Receveur, Marie Grimstrup
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Publication number: 20080114040Abstract: Epothilone derivatives of Formula (I) and their use as a pharmaceutical.Type: ApplicationFiled: March 15, 2005Publication date: May 15, 2008Applicant: NOVARTIS AGInventor: Karl-Heinz Altmann
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Publication number: 20080103185Abstract: There are provided crystals of a thiazolidinedione derivative having excellent prophylactic and therapeutic effects on a disease caused by insulin resistance and a process for producing the thiazolidinedione derivative with a high purity.Type: ApplicationFiled: January 24, 2006Publication date: May 1, 2008Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Yoshitaka Nakamura, Chiharu Satoh, Hiroshi Miyamoto, Hisaki Kajino
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Patent number: 7348425Abstract: Indole compounds of Formula I are described. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.Type: GrantFiled: February 3, 2006Date of Patent: March 25, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Thomas W. Hudyma, Xiaofan Zheng, Feng He, Min Ding, Carl P. Bergstrom, Piyasena Hewawasam, Scott W. Martin, Robert G. Gentles
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Patent number: 7342041Abstract: The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.Type: GrantFiled: February 24, 2005Date of Patent: March 11, 2008Assignee: Schering CorporationInventors: F. George Njoroge, Srikanth Venkatraman, Ashok Arasappan, Francisco Velazquez, Viyyoor M. Girijavallabhan
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Patent number: 7342030Abstract: The present invention relates to the compounds of formula I: their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, compositions containing such compounds and their manufacture, as well as the use of such compounds in the control or prevention of illnesses such as cancer.Type: GrantFiled: September 20, 2005Date of Patent: March 11, 2008Assignee: Hoffmann-La Roche Inc.Inventors: Thomas Friess, Ulrike Reiff, Matthias Rueth, Edgar Voss
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Publication number: 20070203210Abstract: The invention is directed to compounds of formula (1) and pharmaceutically acceptable salts thereof, methods for the preparation thereof, and methods of use thereof.Type: ApplicationFiled: February 7, 2007Publication date: August 30, 2007Inventors: John Frederick Boylan, Jianping Cai, Nader Fotouhi, Paul Gillespie, Robert Alan Goodnow, Kang Le, Christophe Michoud
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Patent number: 7262200Abstract: The present invention provides compounds of formula I: These compounds, and pharmaceutically acceptable compositions thereof, are useful generally as kinase inhibitors, particularly as inhibitors of PRAK, GSK3, ERK2, CDK2, MK2, SRC, SYK, and Aurora-2. Accordingly, compounds and compositions of the invention are useful for treating or lessening the severity of a variety of disorders, including, but not limited to, heart disease, diabetes, Alzheimer's disease, immunodeficiency disorders, inflammatory diseases, allergic diseases, autoimmune diseases, destructive bone disorders such as osteoporosis, proliferative disorders, infectious diseases and viral diseases.Type: GrantFiled: October 27, 2003Date of Patent: August 28, 2007Assignee: Vertex Pharmaceuticals IncorporatedInventors: Alex Aronov, David J. Lauffer, Huan Qui Li, Ronald Charles Tomlinson, Pan Li
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Publication number: 20070191313Abstract: The invention provides compounds represented by the formula I, each of which compounds may have sphingosine-1-phosphate receptor agonist and or antagonist biological activity: and wherein the variables Y, R4, n, A, X, Z, R1, o, R3, R2 and p are as defined in the specification.Type: ApplicationFiled: February 15, 2007Publication date: August 16, 2007Inventors: Richard L. Beard, John E. Donello, Haiqing Yuan, Diana F. Colon, Tien Duong, Xiaoxia Liu, Yihui Hu
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Publication number: 20070167622Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, type II diabetes mellitus and metabolic syndrome.Type: ApplicationFiled: January 8, 2007Publication date: July 19, 2007Inventors: Paul Gillespie, Robert Alan Goodnow, Agnieszka Kowalczyk, Kang Le, Qiang Zhang
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Publication number: 20070166871Abstract: Disclosed herein are NPN-type low molecular aromatic ring compounds, organic semiconductor layers formed from such compounds that exhibit improved electrical stability and methods of forming such layers using solution-based processes, for example, spin coating processes performed at or near room temperature. These NPN-type compounds may be used, either singly or in combination, for fabricating organic semiconductor layers in electronic devices. The NPN-type aromatic ring compounds according to example embodiments may be deposited as a solution on a range of substrates to form a coating film that is then subjected to a thermal treatment to form a semiconductor thin film across large substrate surfaces that exhibits reduced leakage currents relative to conventional PNP-type organic semiconductor materials, thus improving the electrical properties of the resulting devices.Type: ApplicationFiled: August 24, 2006Publication date: July 19, 2007Inventors: Eun Jeong Jeong, Joo Young Kim, Hyun Sik Moon, Bang Lin Lee, Kook Min Han, Eun Kyung Lee
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Patent number: 7241899Abstract: The present invention relates to improved methods for the production, isolation and purification of epothilone B. These methods include, for example, a fermentation process for the production of epothilone B, isolation via adsorption onto a resin, and subsequent purification.Type: GrantFiled: March 22, 2004Date of Patent: July 10, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Daniel A. Benigni, Jack Z. Gougoutas, John D. DiMarco
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Patent number: 7235572Abstract: This invention relates to compounds of the formula wherein one of R6, R7 or R8 is and all enantiomers and pharmaceutically acceptable salts and/or esters thereof as well as pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are modulated by PPAR? and/or PPAR? agonists.Type: GrantFiled: June 28, 2004Date of Patent: June 26, 2007Assignee: Hoffman-La Roche Inc.Inventors: Jean Ackermann, Johannes Aebi, Alfred Binggeli, Uwe Grether, Georges Hirth, Bernd Kuhn, Hans-Peter Maerki, Markus Meyer, Peter Mohr, Matthew Blake Wright
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Patent number: 7205330Abstract: The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.Type: GrantFiled: February 24, 2005Date of Patent: April 17, 2007Assignee: Schering CorporationInventors: Stephane L. Bogen, Weidong Pan, Sumei Ruan, Kevin X. Chen, Ashok Arasappan, Srikanth Venkatraman, Latha G. Nair, Mousumi Sannigrahi, Frank Bennett, Anil K. Saksena, F. George Njoroge, Viyyoor M. Girijavallabhan
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Patent number: 7205406Abstract: An azomethine dye represented by the following Formula 1: wherein Y represents a substituent of 0.2??p?0.9, Z1 and Z2 each represent —CR1?, where R1 represents a hydrogen atom or a substituent, or —N?, L represents the group represented by the following Formula 1a, X represents an unsubstituted or substituted di-alkylamino group, R represents an unsubstituted or substituted alkyl group, and n represents an integer more than 0. wherein B represents a group of non-metallic atoms which are necessary to form a heterocyclic ring.Type: GrantFiled: July 1, 2005Date of Patent: April 17, 2007Assignee: Konica Minolta Holdings, Inc.Inventors: Emiko Kataoka, Takatugu Suzuki, Dai Ikemizu
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Patent number: 7166715Abstract: The invention provides an asymmetric cyanine dye compound having the structure including substituted forms thereof, wherein, at least one of R1 and R2 is linking group, X is O, S, or Se, and n ranges from 0 to 2. The invention further provides reporter-quencher dye pairs comprising the asymmetric cyanine dyes, dye-labelled polynucleotides incorporating the asymmetric cyanine dyes, and hybridization detection methods utilizing the dye-labelled polynucleotides.Type: GrantFiled: May 5, 2004Date of Patent: January 23, 2007Assignee: Applera CorporationInventors: Linda G. Lee, Ronald J. Graham, Khairuzzaman B. Mullah, Francis T. Haxo
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Patent number: 7157585Abstract: Compounds of formula (I) where R5, R6a, each X, L, Cy and Lp are as defined in the specification, are tryptase inhibitors useful as antiinflammatory agents.Type: GrantFiled: May 11, 2005Date of Patent: January 2, 2007Assignee: Tularik LimitedInventors: Sarah Elizabeth Lively, Bohdan Waszkowycz, Martin James Harrison, Christopher Neil Farthing, Keith Michael Johnson
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Patent number: 7153848Abstract: Indole compounds of Formula I are described. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV. Different forms and compositions comprising the compounds are also described as well as methods of preparing the compounds.Type: GrantFiled: July 14, 2005Date of Patent: December 26, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Thomas W. Hudyma, Xiaofan Zheng, Feng He, Min Ding, Carl P. Bergstrom, Piyasena Hewawasam, Scott W. Martin, Robert G. Gentles
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Patent number: 7144903Abstract: Compounds, compositions and methods are provided that are useful in the treatment of chemokine receptor-mediated conditions and diseases. In particular, the invention provides compounds which modulate CCR4 function or a CCR4-mediated response. The subject compounds and compositions are useful for the treatment or prevention of inflammatory conditions and diseases.Type: GrantFiled: May 22, 2002Date of Patent: December 5, 2006Assignee: Amgen Inc.Inventors: Tassie Collins, Hossen Mahmud, Jonathan Houze, Alan Xi Huang, Julio C. Medina, Xuemei Wang, Feng Xu, Qingge Xu, Liusheng Zhu
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Patent number: 7141672Abstract: This invention provides compounds of Formula I having the structure or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.Type: GrantFiled: January 8, 2004Date of Patent: November 28, 2006Assignee: WyethInventor: Michael S. Malamas
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Patent number: 7122674Abstract: The invention relates to a process for preparing hydroxyindolylglyoxylamides in high yields and particularly pure form.Type: GrantFiled: July 31, 2003Date of Patent: October 17, 2006Assignee: Elbion AGInventors: Hans-Joachim Jänsch, Helge Hartenhauer, Hans Stange, Norbert Höfgen, Jürgen Schäfer
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Patent number: 7119209Abstract: The present invention refers to a process for preparing indolinone derivatives of the general formula (VI) as defined in the specification and intermediates of that process.Type: GrantFiled: February 14, 2003Date of Patent: October 10, 2006Assignee: Pharmacia & Upjohn CompanyInventors: Qingwu Jin, Michael A. Mauragis, Paul D. May
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Patent number: RE39356Abstract: The present invention relates to a process for the preparation of epothilone analogs by initially forming novel ring-opened epothilones and carrying out a macrolactamization reaction thereon. The subject process is amenable to being carried out in a single reaction vessel without isolation of the intermediate compound and provides at least about a three-fold increase in yield over prior processes for preparing the desired epothilone analogs.Type: GrantFiled: February 11, 2005Date of Patent: October 17, 2006Assignee: Bristol-Myers Squibb Co.Inventors: Wen Sen Li, John E. Thornton, Zhenrong Guo, Shankar Swaminathan, Robert M. Borzilleri, Soong-Hoon Kim, Denis Favreau