At Least Three Ring Hetero Atoms In The Polycyclo Ring System Patents (Class 548/218)
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Publication number: 20110150827Abstract: Provided herein are 5,5-fused heteroarylene hepatitis C virus inhibitor compounds, for example, of Formula I, IA, or IB, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.Type: ApplicationFiled: December 17, 2010Publication date: June 23, 2011Applicant: Idenix Pharmaceuticals, Inc.Inventors: Cyril B. Dousson, David Dukhan, Christophe Claude Parsy, Claire Pierra, Francois-Rene Alexandre, Guillaume Brandt, Daniel Da Costa, Houcine Rahali, Jean-Laurent Paparin, Michel Derock, Thierry Convard, Dominique Surleraux
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Patent number: 7964598Abstract: The present invention provides compounds that inhibit apoE4 domain interaction; and compositions, including pharmaceutical compositions, comprising the compounds. The present invention provides methods of treating apoE4-related disorders. The methods generally involve administering to an individual in need thereof a therapeutically effective amount of an apoE4 domain interaction inhibitor.Type: GrantFiled: October 4, 2005Date of Patent: June 21, 2011Assignee: The J. David Gladstone InstitutesInventors: Robert W. Mahley, Karl H. Weisgraber, Yadong Huang
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Publication number: 20110137037Abstract: This invention relates to prodrugs of caspase inhibitors comprising of a furo[3,2-d]oxazolin-5-one moiety which, under specific conditions, can convert into biologically active compounds, particularly caspase inhibitors. This invention also relates to the processes for preparing these prodrugs of caspase inhibitors. This invention further relates to pharmaceutical compositions comprising said prodrugs and to the use thereof for the treatment of diseases related to inflammatory or degenerative conditions.Type: ApplicationFiled: December 17, 2010Publication date: June 9, 2011Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Steven Durrant, Jean-Damien Charrier, John Studley
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Publication number: 20110105762Abstract: The present invention relates to certain compounds and to methods for the preparation of certain compounds that can be used in the fields of chemistry and medicine. Specifically, described herein are methods for the preparation of various compounds and intermediates, and the compounds and intermediates themselves. More specifically, described herein are methods for synthesizing Salinosporamide A and its analogs from a compound of formula (V).Type: ApplicationFiled: October 27, 2010Publication date: May 5, 2011Applicant: NEREUS PHARMACEUTICALS, INC.Inventors: Taotao Ling, Venkata Rami Reddy Macherla, Barbara Christine Potts, Rama Rao Manam, Katherine A. McArthur
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Publication number: 20110098327Abstract: This disclosure concerns novel compounds of Formula (I) or Formula (II) as defined in the specification and compositions comprising such novel compounds. These compounds are useful antiviral agents, especially in inhibiting the function of the NS5A protein encoded by Hepatitis C virus (HCV). Thus, the disclosure also concerns a method of treating HCV related diseases or conditions by use of these novel compounds or a composition comprising such novel compounds.Type: ApplicationFiled: April 7, 2010Publication date: April 28, 2011Inventors: Rico Lavoie, John A. Bender, Carol Bachand, Edward H. Ruediger, John F. Kadow
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Publication number: 20110065669Abstract: The present invention is directed to oxazolobenzimidazole derivatives which are potentiators of metabotropic glutamate receptors, particularly 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: May 8, 2009Publication date: March 17, 2011Applicant: Merck Sharp & Dohme Corp.Inventors: Edward J. Brnardic, Mark E. Fraley, Robert M. Garbaccio
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Publication number: 20110065703Abstract: The present invention includes a group of chemical compounds useful as modulators of calcium ion (Ca2+) channels, especially for T-type, N-Type and L-type channels. The present invention also includes pharmaceutical compositions comprising these calcium ion channel modulating agents and methods of using these calcium ion channel modulating agents for the treatment diseases and conditions associated with the calcium ion channels.Type: ApplicationFiled: March 12, 2008Publication date: March 17, 2011Inventor: Jay Jie-Qiang Wu
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Patent number: 7906649Abstract: The present invention is directed to novel substituted aminocyclohexanes which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DPP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. 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 the dipeptidyl peptidase-IV enzyme is involved.Type: GrantFiled: May 19, 2006Date of Patent: March 15, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Tesfaye Biftu, Danqing Feng, Xiaoxia Qian, Ann E. Weber, Jason Cox
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Patent number: 7902376Abstract: A novel process is provided for the preparation of chiral trans-2,3-disubstituted 5-oxotetrahydropyrans of structural formula (I): wherein Ar is optionally substituted phenyl and P is a primary amine protecting group. These compounds are useful in the synthesis of dipeptidyl peptidase-IV inhibitors for the treatment of Type 2 diabetes. Also provided are useful intermediates obtained from the process.Type: GrantFiled: January 22, 2009Date of Patent: March 8, 2011Assignees: Merck Sharp & Dohme Corp., Banyu Pharmaceutical Co., Ltd.Inventors: Feng Xu, Mary M. Kim, Yoshinori Kohmura, Tricia Sladicka, Jonathan D. Rosen, Michael J. Zacuto
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Patent number: 7902196Abstract: The syntheses of the natural products, avrainvillamide and stephacidin B, are provided. The ?,?-unsaturated nitrone functionality of avrainvillamide and its 3-alkylidene-3H-indole 1-oxide core is shown to covalently and reversibly bond to heteroatom-based nucleophiles. This capability may allow these molecules to bind active site nucleophiles and may provide the basis for designing potent and selective enzyme inhibitors. Both avrainvillamide and its dimer stephacidin B have been reported to exhibit antiproliferative activity, and avrainvillamide has been reported to exhibit antimicrobial activity against multi-drug resistant bacteria. Avrainvillamide has been found to target cytoskeleton-linking membrane protein (CLIMP-63) thereby preventing cells from undergoing mitosis. The invention provides syntheses of these natural products as well as analogs of these natural products and their functional cores.Type: GrantFiled: March 17, 2006Date of Patent: March 8, 2011Assignee: President and Fellows of Harvard CollegeInventors: Andrew G. Myers, Seth B. Herzon, Jeremy Earle Wulff, Romain Siegrist, Jakub Svenda, Matthew Allen Zajac
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Patent number: 7893160Abstract: Crosslinkable substituted fluorene compounds; oligomers and polymers prepared from such crosslinkable compounds; films and coatings; and multilayer electronic devices comprising such films are disclosed.Type: GrantFiled: October 25, 2004Date of Patent: February 22, 2011Assignee: Sumitomo Chemical Company, LimitedInventors: Michael Inbasekaran, Wanglin Yu
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Publication number: 20110028730Abstract: The use of cyclic compounds of the formula (I) where n is a number in the range from 1 to 7, X—Y—Z, in each case independently of one another, is O—C?N, N?C—O, NR5—C?N, N?C—NR5, N+R52—C?N, N?C—N+R52, O—C?N+R5, N+R5?C—O, S—C?N+R5, N+R5?C—S, S—C?N, N?C—S, R1, R2 and R3 each independently are, for example, H or a substituent or corresponding heterocyclic compounds in which at least one group —CR1?, —CR2?, CR3? is replaced by —N, R5 in each case independently are, for example, H or a substituent R7 in each case independently of one another, are H, C1-12-alkyl or C6-12-aryl, or metal complexes of the cyclic compounds or complexes of the cyclic compounds with mineral acids, chloride, sulfate, bisulfate, phosphate, hydrogen phosphate, nitrate, BF4? or methanesulfonate being present as opposite ions X? in the case of cationic cyclic structures, as light absorbers, materials for hole injection layers in OLEDs, light-emitting compounds in OLED, phase-transfer catalysts or synergistic agents for the dispersingType: ApplicationFiled: October 4, 2010Publication date: February 3, 2011Applicant: BASF AktiengesellschaftInventors: Martin Könemann, Thomas Geßner, Rüdiger Sens, Christian Lennartz, Günther Seybold
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Patent number: 7879891Abstract: This invention relates to prodrugs of caspase inhibitors comprising of a furo[3,2-d]oxazolin-5-one moiety which, under specific conditions, can convert into biologically active compounds, particularly caspase inhibitors. This invention also relates to the processes for preparing these prodrugs of caspase inhibitors. This invention further relates to pharmaceutical compositions comprising said prodrugs and to the use thereof for the treatment of diseases related to inflammatory or degenerative conditions.Type: GrantFiled: July 20, 2006Date of Patent: February 1, 2011Assignee: Vertex Pharmaceuticals IncorporatedInventors: Steven Durrant, Jean-Damien Charrier, John Studley
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Publication number: 20110021784Abstract: This invention relates to novel macrocyclic lactams intermediates useful for the preparation of diazonamide analogs. This invention also relates to a novel electrochemical oxidative cyclization for the preparation of such macrocyclic lactams, and their further elucidation to provide diazonamide analogs.Type: ApplicationFiled: October 3, 2010Publication date: January 27, 2011Inventors: Gunnar Hanson, Charles Caldwell, Patrick G. Harran, Susan Harran, Qi Wei, Ming Zhou
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Publication number: 20100323963Abstract: The present invention provides conjugates of disorazoles and their derivatives with cell-binding molecules, such as peptides, proteins, hormones, blood proteins and antibodies. The present invention further provides novel disorazole derivatives and processes of manufacturing such conjugates and disorazole derivatives. These compounds can be used as medicaments for the treatment of physiological and/or pathophysiological conditions in mammals, in particular for the treatment of various tumors.Type: ApplicationFiled: March 19, 2010Publication date: December 23, 2010Applicant: AETERNA ZENTARIS GmbHInventors: Eckhard GUENTHER, Olaf Schaefer, Michael Teifel, Klaus Paulini
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Patent number: 7851620Abstract: This invention relates to novel macrocyclic lactams intermediates useful for the preparation of diazonamide analogs. This invention also relates to a novel electrochemical oxidative cyclization for the preparation of such macrocyclic lactams, and their further elucidation to provide diazonamide analogs.Type: GrantFiled: June 6, 2008Date of Patent: December 14, 2010Assignees: Board of Regents, The University of Texas System, Joyant Pharmaceuticals, Inc.Inventors: Gunnar Hanson, Charles Caldwell, Patrick G. Harran, Susan Harran, Qi Wei, Ming Zhou
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Patent number: 7842814Abstract: The present invention relates to certain compounds and to methods for the preparation of certain compounds that can be used in the fields of chemistry and medicine. Specifically, described herein are methods for the preparation of various compounds and intermediates, and the compounds and intermediates themselves. More specifically, described herein are methods for synthesizing Salinosporamide A and its analogs from a compound of formula (V).Type: GrantFiled: April 6, 2007Date of Patent: November 30, 2010Assignee: Nereus Pharmaceuticals, Inc.Inventors: Taotao Ling, Venkata Rami Reddy Macherla, Barbara Christine Potts, Rama Rao Manam, Katherine A. McArthur
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Publication number: 20100292190Abstract: The present invention relates to compounds of general formula (I) as tublin polymerisation inhibitors and methods for preparing such compounds.Type: ApplicationFiled: February 14, 2006Publication date: November 18, 2010Applicant: Bionomics LimitedInventors: Jason Hugh Chaplin, Gurmit Singh Gill, Damian Wojciech Grobelny, Bernard Luke Flynn
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Patent number: 7812173Abstract: The present disclosure relates to the preparation and use of tetrahydro-1,8-dioxa-4a-aza-naphthalenes in low VOC coatings.Type: GrantFiled: August 17, 2006Date of Patent: October 12, 2010Assignee: E.I. du Pont de Nemours and CompanyInventors: Neville Everton Drysdale, Laura Ann Lewin
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Patent number: 7790741Abstract: The present invention is directed to novel compounds of formula (I) wherein the variables are as defined herein. The compounds of formula (I) are useful as kinase inhibitors and as such would be useful in treating certain conditions and diseases, especially inflammatory conditions and diseases and proliferative disorders and conditions, for example, cancers.Type: GrantFiled: October 5, 2007Date of Patent: September 7, 2010Assignee: Abbott LaboratoriesInventors: David J. Calderwood, Kristine E. Frank, David W. Borhani, Heather M. Davis, Nathan S. Josephsohn, Barbara S. Skinner
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Patent number: 7750034Abstract: The present invention is directed to novel substituted aminocyclohexanes of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. 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 the dipeptidyl peptidase-IV enzyme is involved.Type: GrantFiled: January 19, 2007Date of Patent: July 6, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Tesfaye Biftu, Jason Cox, Danqing Feng, Anthony Mastracchio, Xiaoxia Qian, Ann E. Weber
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Patent number: 7749994Abstract: The invention provides novel kinase inhibitors that are useful as therapeutic agents for example in the treatment malignancies where the compounds have the general formula I wherein A, X, Y, Z, Ra, Rb, Rc, R1, R2, R3 and m are defined herein.Type: GrantFiled: August 14, 2006Date of Patent: July 6, 2010Assignees: Genentech, Inc., Hoffman-LaRoche, Inc. (US Only), F. Hoffman-LaRoche, AG (EX-US)Inventors: Thomas E. Rawson, Brian Safina, Jennafer Dotson, Aihe Zhou, Ignacio Aliagas-Martin, Jason Halladay, Jun Liang, Matthias Rueth, Bing-Yan Zhu, Frederick Brookfield, Michael Prime, Birong Zhang, Jun M. Li
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Publication number: 20100163813Abstract: The instant invention relates to novel benzotriazole UV-absorbers having a long wavelength shifted absorption spectrum with significant absorbance up to 410-420 nm. Further aspects of the invention are a process for their preparation, a UV stabilized composition containing the new UV-absorbers and the use of the new compounds as UV-light stabilizers for organic materials.Type: ApplicationFiled: June 18, 2007Publication date: July 1, 2010Inventors: Katharina Fritzsche, Markus Grob, Adalbert Braig, Iloan Marion Kienzle, Gérard Daniel Georges Vilain
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Publication number: 20100160330Abstract: The present invention is directed to novel bicyclic heterocycles, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.Type: ApplicationFiled: October 15, 2009Publication date: June 24, 2010Inventors: Xuqing Zhang, Zhihua Sui
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Patent number: 7741343Abstract: Compounds of the formula I in which R1, R2, R3 and R4 are as defined in Claim 1, are ligands of the nicotinic acetylcholine receptor and/or serotonergic ligands and are suitable for the prophylaxis or treatment of psychoses, schizophrenia, depression, anxiety states, dementia, in particular Alzheimer's disease and Lewy bodies dementia, neurodegenerative disorders, Parkinson's disease, amyotrophic lateral sclerosis, Huntington's disease, Tourette's syndrome, learning and memory restrictions, bulimia, anorexia nervosa or other eating disorders, compulsive behavior, premenstrual syndrome, age-induced memory impairment, amelioration of withdrawal symptoms in nicotine dependence, strokes or brain damage by toxic compounds, and for the treatment of disorders which are characterized by an excess of circulating serotonin or by serotonergic hyperactivity.Type: GrantFiled: October 30, 2007Date of Patent: June 22, 2010Assignee: Merck Patent GmbHInventors: Kai Schiemann, Henning Böttcher, Joachim Leibrock
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Patent number: 7732435Abstract: The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, in free form or in salt form, to their preparation, to their use as medicaments and to medicaments comprising them.Type: GrantFiled: December 5, 2006Date of Patent: June 8, 2010Assignee: Novartis AGInventors: Andrew James Culshaw, Christopher Thomas Brain, Edward Karol Dziadulewicz, Lee Edwards, Terance William Hart, Timothy John Ritchie
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Publication number: 20100069374Abstract: This invention relates to benzopyran derivatives of formula (I) or (II), or pharmaceutically acceptable salts thereof wherein R1 and R2 are independently of each other hydrogen atom, C1-6alkyl group or C6-14aryl group, R3 is hydrogen atom or C1-6alkylcarbonyloxy group, or together with R4 forms a bond, R4 is hydrogen atom, or together with R3 forms a bond, m is an integer of 0 to 4, n is an integer of 0 to 4, V is a single bond, CR7R8, NR9, O, S, SO or SO2, R5 is hydrogen atom or C1-6alkyl group, R6 is hydrogen atom, C1-6alkyl group, C3-8cycloalkyl group, C3-8cycloalkenyl group, amino group, C1-6alkylamino group, di-C1-6alkylamino group, C6-14arylamino group, C2-9heteroarylamino group, C6-14aryl group, C2-9heteroaryl group or C2-9heterocyclyl group, A is 5-, 6- or 7-member ring fused with benzene ring, as constituent atom of the ring, oxygen atom, nitrogen atom or sulfur atom may be contained in the number of 1 to 3 alone or in a combination thereof, the number of unsaturated bond in the ring is 1, 2 or 3Type: ApplicationFiled: November 17, 2009Publication date: March 18, 2010Applicant: NISSAN CHEMICAL INDUSTRIES, LTD.Inventors: Kazuhiko Ohrai, Yukohiro Shigeta, Osamu Uesugi, Takumi Okada, Tomoyuki Matsuda
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Patent number: 7666864Abstract: The current invention provides a series of bicyclic nitroimidazole-substituted phenyl oxazolidinones in which a bicyclic nitroimidazole pharmacophore is covalently bonded to a phenyl oxazolidinone, their pharmaceutical compositions, and the method of use of the compositions for prevention and treatment of bacterial infections. The bicyclic nitroimidazole-substituted phenyl oxazolidinones possess surprising antibacterial activity against wild-type and resistant strains of pathogens, and are therefore useful for the prevention, control and treatment of a number of human and veterinary bacterial infections caused by these pathogens, such as Mycobacterium tuberculosis.Type: GrantFiled: March 25, 2009Date of Patent: February 23, 2010Assignee: Global Alliance for TB Drug DevelopmentInventors: Charles Z. Ding, Genliang Lu, Keith Combrink, Dianjun D. Chen, Minsoo Song, Jiancheng Wang, Zhenkun Ma, Brian Desmond Palmer, Adrian Blaser, Andrew M. Thompson, Iveta Kmentova, Hamish Scott Sutherland, William Alexander Denny
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Publication number: 20100035874Abstract: There are described pyrazolo[5.1-b]oxazole derivatives useful as corticotropin releasing factor (CRF1) receptor antagonists.Type: ApplicationFiled: August 3, 2009Publication date: February 11, 2010Inventors: Ian Bruce, Andrew James Culshaw, Nicholas James Devereux, François Gessier, Jeffrey Mc Kenna, James Neef, Helen Elizabeth Oakman
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Publication number: 20090270467Abstract: The present invention is directed to novel substituted aminocyclohexanes of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. 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 the dipeptidyl peptidase-IV enzyme is involved.Type: ApplicationFiled: January 19, 2007Publication date: October 29, 2009Applicant: MERCK & CO., INC.Inventors: Tesfaye Biftu, Jason Cox, Danqing Feng, Anthony Mastracchio, Xiaoxia Qian, Ann E. Weber
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Patent number: 7598282Abstract: Novel stereoisomers of GS-164 are provided. The compounds, such as (3R,5S,7as)-(3,5-bis(4-fluorophenyl)tetrahydro-1H-oxazolo[3,4-c]oxazol-7a-yl)methanol (TH-237A) and (3R,5S,7as)-(3,5-bis(4-fluorophenyl)tetrahydro-1H-oxazolo[3,4-c]oxazol-7a-yl)methanol (TH-242A) exhibit neuroprotective effects via a mechanism that does not involve microtubule stabilization.Type: GrantFiled: November 1, 2006Date of Patent: October 6, 2009Assignee: University of KansasInventors: Mary Louise Michaelis, Ingrid Gunda Georg, Richard H. Himes, Kenneth L. Audus
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Publication number: 20090209593Abstract: This invention relates to novel macrolides, to the preparation of novel macrolides, to the use of such novel macrolides for preventing, treating, or ameliorating various conditions, and to the use of such novel macrolides as antibacterial agents.Type: ApplicationFiled: April 27, 2009Publication date: August 20, 2009Inventors: Chang-Hsing Liang, Jonathan Duffield, Alex Romero, Yu-Hung Chiu, David Rabuka, Sulan Yao, Steve Sucheck, Kenneth Marby, Youe-kong Shue, Yoshi Ichikawa, Chan-Kou Hwang
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Publication number: 20090209547Abstract: The present invention discloses compounds of formula (I) or pharmaceutically acceptable salts, esters, or prodrugs thereof: which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes process by which to make the compounds of the present invention.Type: ApplicationFiled: February 13, 2009Publication date: August 20, 2009Inventors: IN JONG KIM, GUOQIANG WANG, HEEJIN KIM, YAT SUN OR
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Publication number: 20090187028Abstract: A novel process is provided for the preparation of chiral trans-2,3-disubstituted 5-oxotetrahydropyrans of structural formula (I): wherein Ar is optionally substituted phenyl and P is a primary amine protecting group. These compounds are useful in the synthesis of dipeptidyl peptidase-IV inhibitors for the treatment of Type 2 diabetes. Also provided are useful intermediates obtained from the process.Type: ApplicationFiled: January 22, 2009Publication date: July 23, 2009Inventors: Feng Xu, Mary M. Kim, Yoshinori Kohmura, Tricia Sladicka, Jonathan D. Rosen, Michael J. Zacuto
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Patent number: 7504440Abstract: The present invention relates to novel poly(meth)acrylate compositions formed by polymerization of (meth)acrylate amide acetals.Type: GrantFiled: September 30, 2005Date of Patent: March 17, 2009Assignee: E.I. du Pont de Nemours & CompanyInventors: Neville Everton Drysdale, Laura Ann Lewin, Robert John Barsotti, Patrick Henry Corcoran
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Publication number: 20090005572Abstract: This invention relates to novel macrocyclic lactams intermediates useful for the preparation of diazonamide analogs. This invention also relates to a novel electrochemical oxidative cyclization for the preparation of such macrocyclic lactams, and their further elucidation to provide diazonamide analogs.Type: ApplicationFiled: June 6, 2008Publication date: January 1, 2009Inventors: Gunnar HANSON, Charles CALDWELL, Patrick G. HARRAN, Susan HARRAN, Qi WEI, Ming ZHOU
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Publication number: 20080305063Abstract: 1-aza-3,7-dioxabicyclo[3.3.0]octane compounds, process for their preparation, their use as pro-fragrances, and washing and cleaning compositions, fabric softeners and cosmetics comprising them, and a process for prolonging the odor perception of such compositions.Type: ApplicationFiled: July 17, 2008Publication date: December 11, 2008Inventors: Ursula HUCHEL, Silvia SAUF, Thomas GERKE
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Publication number: 20080290329Abstract: Provided are novel hetero-polycyclic compounds having a specific structure, color-changing material compositions comprising (A) a fluorescent coloring matter comprising at least one of the hetero-polycyclic compounds described above and (B) a binder material, color-changing films comprising the above hetero-polycyclic compounds, coloring matters comprising the above hetero-polycyclic compounds, and pigments or dyes comprising the hetero-polycyclic compounds described above, and provided are color-changing material compositions which are not deteriorated in a color-changing performance even after used for long time and which are prevented from being unusable due to deposition of coloring matters during storage and color-changing films produced by using the same, and novel hetero-polycyclic compounds, coloring matters and pigments or dyes which actualize them.Type: ApplicationFiled: July 31, 2008Publication date: November 27, 2008Applicants: Idemitsu Kosan Co., Ltd., TECHNO NETWORK SHIKOKU CO., LTD.Inventors: Katsuhira YOSHIDA, Yousuke Ooyama, Satoshi Hachiya
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Publication number: 20080161341Abstract: The present invention is directed to novel compounds of formula (I) wherein the variables are as defined herein. The compounds of formula (I) are useful as kinase inhibitors and as such would be useful in treating certain conditions and diseases, especially inflammatory conditions and diseases and proliferative disorders and conditions, for example, cancers.Type: ApplicationFiled: October 5, 2007Publication date: July 3, 2008Inventors: David J. Calderwood, Kristine E. Frank, David W. Borhani, Heather M. Davis, Nathan S. Josephsohn, Barbara S. Skinner
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Patent number: 7390875Abstract: The invention concerns a method for binding, in solution, at least a peptide composition and at least a lipophilic vector bearing an aldehyde function, the coupling comprising a step which consists in producing a hydrazone bond between the peptide compound and the lipophilic vector. The invention also concerns lipophilic vectors for use in this method, lipopeptides obtained by this method, uses of the lipopeptides for cell screening, and the applications of the invention, in particular for preparing targeting of an active principle of the peptide kind (for example hormone or neuropeptide) through physiological barriers such as cell membranes.Type: GrantFiled: September 7, 2001Date of Patent: June 24, 2008Assignee: Institut Pasteur de LilleInventors: Dominique Bonnet, Line Bourel, Oleg Melnyk, Hélène Gras-Masse
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Patent number: 7378431Abstract: Compounds having NR2B selective NMDA receptor antagonist activity are disclosed of the formula (I) wherein one of the neighboring R1, R2, R3 and R4 groups is hydroxy, and the others are each hydrogen atoms, R5 and R6 together with the nitrogen between them form a saturated or unsaturated, 4-6 membered heterocyclic ring, which is substituted by phenoxy, phenyl-(C1-C4 alkyl), phenyl-(C1-C4 alkoxy), phenoxy-(C1-C4 alkyl), or benzoyl, optionally substituted on the aromatic ring by one or more halogen atoms, cyano or hydroxy groups, C1-C4 alkyl or C1-C4 alkoxy groups, X is NH—, Y is a nitrogen atom, or pharmaceutically acceptable salts thereof formed with acids or bases.Type: GrantFiled: December 29, 2004Date of Patent: May 27, 2008Assignee: Richter Gedeon Vegyeszeti Gyar Rt.Inventors: Csilla Horvath, Sandor Farkas, György Domany, Istvan Borza, Gizella Bartane Szalai, Jozsef Nagy, Sandor Kolok
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Publication number: 20080119478Abstract: The present invention provides a 2,3-dihydro-6-nitroimidazo[2,1-b]oxazole compound represented by the following general formula: (1) in the above formula (1), R1 represents a hydrogen atom or C1-C6 alkyl group, n represents an integer of 0 to 6, R1 and —(CH2)nR2 may form a spiro ring represented by the formula (30) below, together with the adjacent carbon atom (in the formula below, RRR represents a piperidyl group which may have substituents on the piperidine ring), (30) and R2 represents a benzothiazolyloxy group, quinolyloxy group, pyridyloxy group or the like. The present compound has an excellent bactericidal action against Mycobacterium tuberculosis, multi-drug-resistant Mycobacterium tuberculosis, and atypical acid-fast bacteria.Type: ApplicationFiled: October 29, 2004Publication date: May 22, 2008Inventors: Hidetsugu Tsubouchi, Hirofumi Sasaki, Motohiro Itotani, Yoshikazu Haraguchi, Shin Miyamura, Makoto Matsumoto, Hiroyuki Hashizume, Tatsuo Tomishige, Masanori Kawasaki, Kinue Ohguro, Takumi Sumida, Takeshi Hasegawa, Kazuho Tanaka, Isao Takemura
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Patent number: 7375116Abstract: Compounds having NR2B selective NMDA receptor antagonist activity are disclosed of the formula (I) where two of the neighboring R1, R2, R3 and R4 groups form an imidazole ring fused to the benzene ring of the indole nucleus, and the other two of R1, R2, R3 and R4 groups are hydrogen atoms, R5 and R6 together with the nitrogen between them form a saturated or unsaturated, 4-6 membered heterocyclic ring, which is substituted by phenoxy, phenyl-(C1-C4 alkyl), phenyl-(C1-C4 alkoxy), phenoxy-(C1-C4 alkyl), or benzoyl, optionally substituted on the aromatic ring by one or more halogen atoms, cyano or hydroxy groups, C1-C4 alkyl or C1-C4 alkoxy groups, X is NH—, Y is a —CH— group, or pharmaceutically acceptable salts thereof formed with acids or bases.Type: GrantFiled: December 29, 2004Date of Patent: May 20, 2008Assignee: Richter Gedeon Vegyeszeti Gyar RT.Inventors: Csilla Horvath, Sandor Farkas, György Domany, Istvan Borza, Gizella Bartane Szalai, Jozsef Nagy, Sandor Kolok
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Patent number: 7365083Abstract: Compounds having NR2B selective NMDA receptor antagonist activity are disclosed of the formula (I) wherein two of the neighboring R1, R2, R3 and R4 groups form an oxo-oxazolidine ring fused to the benzene ring of the indole nucleus, and the other two of R1, R2, R3 and R4 groups are hydrogen atoms, R5 and R6 together with the nitrogen between them form a saturated or unsaturated, 4-6 membered heterocyclic ring, which is substituted by phenoxy, phenyl-(C1-C4 alkyl), phenyl-(C1-C4 alkoxy), phenoxy-(C1-C4 alkyl), or benzoyl, optionally substituted on the aromatic ring by one or more halogen atoms, cyano or hydroxy groups, C1-C4 alkyl or C1-C4 alkoxy groups, X is NH—, Y is a —CH— group, or pharmaceutically acceptable salts thereof formed with acids or bases.Type: GrantFiled: December 28, 2004Date of Patent: April 29, 2008Assignee: Richter Gedeon Vegyeszeti Gyar Rt.Inventors: Csilla Horvath, Sandor Farkas, György Domany, Istvan Borza, Gizella Bartane Szalai, Jozsef Nagy, Sandor Kolok
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Patent number: 7358367Abstract: The present invention relates to the new 3-decladinosyl derivatives of 9-de-oxo-9a-aza9a-homoerythromycin A 9a,11-cyclic carbamate of the general formula (I), their pharmaceutically acceptable addition salts with inorganic or organic acids and their hydrates, wherein R1 individually stands for hydrogen, hydroxyl or a group of the formula (II), wherein X individually stands for C1-C6alkyl group, C2-C6alkenyl group or X individually stands for C1-C6alkyl group with at least one incorporated O, S or N atom or X individually stands for (CH2)n—Ar or X individually stands for (CH2)n-heterocycloalkyl, wherein (CH2)n individually stands for alkyl, wherein n is 1-10, with or without incorporated atom O, S or N, wherein Ar individually stands for 5-10-membered monocyclic or bycyclic aromatic ring with 0-3 atom O, S or N, unsubstituted or substituted with 1-3 group, which are selected independently from halogen, OH, OMe, NO2, NH2, amino-C1-C3alkyl or amino-C1-C3dialkyl, CN, SO2NH2, C1-C3alkyl, and heterocycloalkyl standType: GrantFiled: September 26, 2003Date of Patent: April 15, 2008Assignee: GlaxoSmithKline istrazivacki Centar Zagreb d.o.Inventors: Andrea Fajdetic, Gabrijela Kobrehel, Gorjana Lazarevski, Stjepan Mutak
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Patent number: 7355050Abstract: The present invention, in one aspect, is a composition comprising (meth)acrylate amide acetals. Acetals of the present invention are useful as components in coatings for automotive and architectural structures. Coatings comprising components of the present invention cure rapidly with low VOC emissions. In another aspect, the present invention provides a process for making (meth)acrylate amide acetals described herein.Type: GrantFiled: September 30, 2005Date of Patent: April 8, 2008Assignee: E.I. du Pont de Nemours and CompanyInventors: Neville Everton Drysdale, Laura Ann Lewin, Robert John Barsotti, Charles J. Brandenburg
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Patent number: 7354946Abstract: The present invention relates to a compound of Formula (I) and the manufacturing method(s) thereof and the use thereof: Formula (I) wherein: Ar is a nitrogen-containing heteroaromatic ring group; X and Z are each a carbon atom, and so on; Y is CO, and so on; R1 is a hydrogen atom, and so on; R2 and R3 are each a hydrogen atom, and so on; R4 and R5 are each a hydrogen atom, and so on; and the formula is a single bond or a double bond. According to the present invention, the compound of the present invention can provide Cdk4 and/or Cdk6 inhibitors for treating malignant tumors, because the compounds of the present invention exhibit a prominent growth inhibitory activity against tumor cells.Type: GrantFiled: December 3, 2004Date of Patent: April 8, 2008Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Takashi Hayama, Kyoko Hayashi, Teruki Honma, Ikuko Takahashi
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Patent number: 7338720Abstract: An organic electroluminescent (EL) device which uses, as a luminescence-assisting agent, a novel coumarin derivative with a specific structure. The coumarin derivative effectively accelerates in such an organic EL device the transfer of excited energy in a host compound to a guest compound. Thus, the coumarin derivative affords the organic EL device which is superior in a color purity, luminescent efficiency and life expectancy when used in combination with appropriate host and guest compounds.Type: GrantFiled: April 23, 2002Date of Patent: March 4, 2008Assignee: Kabushiki Kaisha Toyota JidoshokkiInventors: Makoto Satsuki, Natsuko Ishida, Sadaharu Suga, Hisayoshi Fujikawa, Yasunori Taga, Satoshi Nakagawa, Takanori Murasaki, Yoshifumi Kato
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Patent number: 7307095Abstract: The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S.Type: GrantFiled: January 5, 2007Date of Patent: December 11, 2007Assignee: IRM LLCInventors: Hong Liu, David Tully, Phillip Alper, Robert Epple, Arnab Chatterjee, Michael Roberts
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Patent number: 7291633Abstract: Compounds of the formula I in which R1, R2, R3 and R4 are as defined in claim 1, are ligands of the nicotinic acetylcholine receptor and/or serotonergic ligands and are suitable for the prophylaxis or treatment of psychoses, schizophrenia, depression, anxiety states, dementia, in particular Alzheimer's disease and Lewy bodies dementia, neurodegenerative disorders, Parkinson's disease, amyotrophic lateral sclerosis, Huntington's disease, Tourette's syndrome, learning and memory restrictions, bulimia anorexia nervosa or other eating disorders, compulsvie behaviour, premenstrual syndrome, age-induced memory impairment, amelioration of withdrawal symptoms in nicotine dependence, strokes or brain damage by toxic compounds, and for the treatment of disorders which are characterised by an excess of circulating serotonin or by serotonergic hyperactivityType: GrantFiled: April 5, 2002Date of Patent: November 6, 2007Assignee: Merck Patent GmbHInventors: Kai Schiemann, Henning Böttcher, Joachim Leibrock