Hetero Ring Is Six-membered Consisting Of One Nitrogen And Five Carbons Patents (Class 546/1)
  • Publication number: 20100055056
    Abstract: The present invention herein provides a compound which promotes drug-permeation into nails. A penetrating promoter comprises, for instance, the following formulas. R1, R2 and R3 are alkyl groups having a carbon number of 1 to 15 and have OH groups at their ends.
    Type: Application
    Filed: September 4, 2008
    Publication date: March 4, 2010
    Applicant: SATO PHARMACEUTICAL CO., LTD.
    Inventors: Masatoshi KATO, Hiroyuki KUSAKABE, Kazuhiro NIMURA, Hiroaki KIMURA, Koh NAGASAWA, Akihiro HASHIGUCHI, Chisato HIROSAWA, Tomohiro TADA
  • Patent number: 7662818
    Abstract: Compounds of the formula (I): wherein A and B together represent an optionally substituted, fused aromatic ring; X can be NRX or CRXRY; if X=NRX then n is 1 or 2 and if X=CRXRY then n is 1; RX is selected from the group consisting of H, optionally substituted C1-20 alkyl, C5-20 aryl, C3-20 heterocyclyl, amido, thioamido, ester, acyl, and sulfonyl groups; RY is selected from H, hydroxy, amino; or RX and RY may together form a spiro-C3-7 cycloalkyl or heterocyclyl group; RC1 and RC2 are both hydrogen, or when X is CRXRY, RC1, RC2, RX and RY, together with the carbon atoms to which they are attached, may form an optionally substituted fused aromatic ring; and R1 is selected from H and halo.
    Type: Grant
    Filed: December 23, 2005
    Date of Patent: February 16, 2010
    Assignees: Kudos Pharmaceuticals Limited, Maybridge Limited
    Inventors: Niall Morrison Barr Martin, Graeme Cameron Smith, Stephen Philip Jackson, Vincent Junior M Loh, Xiao-Ling Fan Cockcroft, Ian Timothy Williams Matthews, Keith Allan Menear, Frank Kerrigan, Alan Ashworth
  • Patent number: 7635792
    Abstract: Polyfluorene polymers and copolymers having substantial amounts (10-100%) of fluorenes coupled at the 2 and 5 positions of fluorene are useful as active layers in OLED devices where triplet energies >2.10 eV are required.
    Type: Grant
    Filed: October 14, 2008
    Date of Patent: December 22, 2009
    Assignee: General Electric Company
    Inventors: James Anthony Cella, Joseph John Shiang, Elliott West Shanklin, Paul Michael Smigelski
  • Patent number: 7629108
    Abstract: A resist composition comprising as a quencher a nitrogen-containing organic compound bearing a nitrogen-containing heterocycle and having a molecular weight of at least 380 exhibits a high resolution and satisfactory mask coverage dependence and is useful in microfabrication using electron beam or deep-UV.
    Type: Grant
    Filed: October 24, 2007
    Date of Patent: December 8, 2009
    Assignee: Shin-Etsu Chemical Co., Ltd.
    Inventors: Takeru Watanabe, Youichi Ohsawa, Masaki Ohashi, Wataru Kusaki, Tomohiro Kobayashi
  • Patent number: 7625917
    Abstract: This invention pertains to the discovery of a novel family of thiolesters and uses thereof. Also provided for are viricidal compounds and pharmaceutical formulations comprising these novel thiolesters. The invention also provides thiolester-inactivated viruses and thiolester-complexed viral proteins.
    Type: Grant
    Filed: December 16, 2003
    Date of Patent: December 1, 2009
    Inventors: James A. Turpin, Yongsheng Song, Ettore Appella, John K. Inman, David G. Covell, William G. Rice, Anders Wallqvist, Andrew Maynard, Mingjun Huang
  • Publication number: 20090258897
    Abstract: Disclosed herein are substituted benzimidazole-based proton pump modulators of Formula I, processes of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Application
    Filed: April 11, 2008
    Publication date: October 15, 2009
    Applicant: Auspex Pharmaceuticals, Inc.
    Inventors: Thomas G. Gant, Sepehr Sarshar
  • Patent number: 7582366
    Abstract: A difluoropyridine-based compound includes at least one difluoropyridine group in its molecule. The difluoropyridine-based compound may be used as an electron injection material, an electron transport material, or a hole blocking material in full-color fluorescent or phosphorescent devices. The difluoropyridine-based compound has good electrical characteristics and a high charge transport capability. The difluoropyridine-based compound may be used to produce an organic electroluminescent device with high efficiency, low voltage, improved brightness, and a long life expectancy.
    Type: Grant
    Filed: March 16, 2006
    Date of Patent: September 1, 2009
    Assignee: Samsung Mobile Display Co., Ltd.
    Inventors: Seok-Hwan Hwang, Young-Kook Kim, Chang-Ho Lee, Seok-Jong Lee, Seung-Gak Yang, Hee-Yeon Kim, Jung-Han Shin
  • Patent number: 7553959
    Abstract: This invention provides for labeling reagents, labeled targets and processes for preparing labeling reagents. The labeling reagents can take the form of cyanine dyes, xanthene dyes, porphyrin dyes, coumarin dyes or composite dyes. These labeling reagents are useful for labeling probes or targets, including nucleic acids and proteins. These reagents can be usefully applied to protein and nucleic acid probe based assays. They are also applicable to real-time detection processes.
    Type: Grant
    Filed: January 23, 2004
    Date of Patent: June 30, 2009
    Assignee: Enzo Life Sciences, Inc.
    Inventors: Jannis G. Stavrianopoulos, Elazar Rabbani
  • Patent number: 7550461
    Abstract: Disclosed are amide compounds of formula (I): wherein Ar1, Q, Y and R3-R6 of formula (I) are defined herein. The compounds inhibit production of cytokines involved in inflammatory processes and are thus useful for treating diseases and pathological conditions involving inflammation such as chronic inflammatory disease. Also disclosed are processes for preparing these compounds and pharmaceutical compositions comprising these compounds.
    Type: Grant
    Filed: April 10, 2003
    Date of Patent: June 23, 2009
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Donghong Amy Gao, Daniel R. Goldberg, Abdelhakim Hammach, Ming-Hong Hao, Victor Marc Kamhi, Neil Moss, Kevin Chungeng Qian, Gregory Paul Roth, Christopher Ronald Sarko, Alan David Swinamer, Zhaoming Xiong
  • Patent number: 7514555
    Abstract: Agents useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyper-lipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis are disclosed.
    Type: Grant
    Filed: April 8, 2004
    Date of Patent: April 7, 2009
    Assignee: Wellstat Therapeutics Corporation
    Inventors: Kirvin L. Hodge, Shalini Sharma, Reid W. von Borstel, Stephen D. Wolpe
  • Patent number: 7507817
    Abstract: Novel compounds, and therapeutic methods, compositions and medicament related thereto are disclosed herein.
    Type: Grant
    Filed: November 13, 2007
    Date of Patent: March 24, 2009
    Assignee: Allergan, Inc.
    Inventors: David W. Old, Vinh X. Ngo, Wha-Bin Im
  • Patent number: 7498436
    Abstract: This present invention relates to prodrug compounds of the formula (Y) and pharmaceutical salts thereof: where RN, R1, R2, R3R4 and RC are defined herein, which are useful in treating Alzheimer's disease and other similar diseases.
    Type: Grant
    Filed: February 27, 2003
    Date of Patent: March 3, 2009
    Assignees: Pharmacia & Upjohn Company LLC, Elan Pharmaceuticals, Inc.
    Inventors: Varghese John, Barbara Jagodzinska, Michel Maillard, James P. Beck, Ruth E. TenBrink, Daniel Getman
  • Publication number: 20090054435
    Abstract: The present invention provides a compound represented by the formula: wherein each symbol is as defined in the specification. Since the compound of the present invention has superior hypoglycemic action and superior hypolipidemic action, it is useful as an agent for the prophylaxis or treatment of diabetes, hyperlipidemia, impaired glucose tolerance and the like.
    Type: Application
    Filed: July 28, 2006
    Publication date: February 26, 2009
    Inventor: Hiroshi Imoto
  • Publication number: 20090053175
    Abstract: 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: Application
    Filed: August 22, 2008
    Publication date: February 26, 2009
    Inventors: Yat Sun Or, Ce Wang, Jiang Long, Lu Ying, Yao-Ling Qiu
  • Patent number: 7482357
    Abstract: Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner. These compounds are useful in the enhancement of weakened muscle tone and the treatment of conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including osteoporosis, osteopenia, glucocorticoid-induced osteoporosis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, postmenopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, obesity, aplastic anemia and other hematopoietic disorders, inflammatory arthritis and joint repair, HIV-wasting, prostate cancer, benign prostatic hyperplasia (BPH), cancer cachexia, Alzheimer's disease, muscular dystrophies, cognitive decline, sexual dysfunction, sleep apnea, depression, premature ovarian failure, and autoimmune disease, alone or in combination with other active agents.
    Type: Grant
    Filed: June 25, 2004
    Date of Patent: January 27, 2009
    Assignee: Merck & Co., Inc.
    Inventors: William P. Dankulich, Mildred L. Kaufman, Robert S. Meissner, Helen J. Mitchell
  • Patent number: 7470702
    Abstract: Novel compounds of the formula I in which R1, R1?, L, E, G, M, Q, U, R2, m, p and q have the meanings indicated. Further, the compounds of formula I can be used as, for example, inhibitors of tyrosine kinases, for example TIE-2 , and can be employed, for example, for the treatment of tumours or other diseases.
    Type: Grant
    Filed: October 14, 2004
    Date of Patent: December 30, 2008
    Assignee: Merck Patent GmbH
    Inventors: Wolfgang Staehle, Hans-Peter Buchstaller, Alfred Jonczyk, Wilfried Rautenberg
  • Patent number: 7455827
    Abstract: Nicotinamides and isonicotinamides, used in the preparation of anti-TB drugs i.e. isoniazid and as an intermediate of vitamin B12 are prepared from cyanopyridines and nicotinamides. Catalysts useful for the preparation of nicotinamide and isonicotinamide.
    Type: Grant
    Filed: January 24, 2006
    Date of Patent: November 25, 2008
    Assignee: Council of Scientific and Industrial Research
    Inventors: Subhash Chandra Ray, Baldev Singh, Hiralal Prasad, Prodyot Kumar Sarkar, Pashupati Dutta, Shyam Kishore Roy, Anup Kumar Bandyopadhyay, Raja Sen
  • Patent number: 7449488
    Abstract: In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of protein and/or checkpoint kinases, methods of preparing such compounds, pharmaceutical compositions including one or more such compounds, methods of preparing pharmaceutical formulations including one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the protein or checkpoint kinases using such compounds or pharmaceutical compositions. The invention also relates to the inhibition of hepatitis C virus (HCV) replication. In particular, embodiments of the invention provide compounds and methods for inhibiting HCV RNA-dependent RNA polymerase enzymatic activity. The invention also provides compositions and methods for the prophylaxis and treatment of HCV infection.
    Type: Grant
    Filed: October 6, 2005
    Date of Patent: November 11, 2008
    Assignee: Schering Corporation
    Inventors: Kamil Paruch, Timothy J. Guzi, Michael P. Dwyer, Gerald W. Shipps, Jr.
  • Patent number: 7446210
    Abstract: The present invention is directed to novel compounds of Formula I: and forms and pharmaceutical compositions thereof, and the use thereof as inhibitors of Factor Xa.
    Type: Grant
    Filed: October 24, 2005
    Date of Patent: November 4, 2008
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Tianbao Lu, Tho V. Thieu, Yu-Kai Lee, Daniel J. Parks, Thomas P. Markotan, Wenxi Pan, Karen L. Milkiewicz, Mark R. Player
  • Patent number: 7442796
    Abstract: Agents useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyper-lipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis are disclosed.
    Type: Grant
    Filed: April 20, 2004
    Date of Patent: October 28, 2008
    Assignee: Wellstat Therapeutics Corporation
    Inventors: Shalini Sharma, Reid W. von Borstel
  • Publication number: 20080251169
    Abstract: An ionic liquid is disclosed A precursor composition that comprises at least one ionic liquid and at least one energetic material is also disclosed, as is a method of synthesizing an ionic liquid and a method of desensitizing an explosive composition.
    Type: Application
    Filed: April 13, 2007
    Publication date: October 16, 2008
    Applicant: ALLIANT TECHSYSTEMS INC.
    Inventors: Steven M. Nicolich, Alexander J. Paraskos, Daniel W. Doll, Gary K. Lund, Wendy A. Balas
  • Patent number: 7435815
    Abstract: The invention relates to novel sulfonylamino-acetic acid derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of such compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as orexin receptor antagonists.
    Type: Grant
    Filed: May 31, 2007
    Date of Patent: October 14, 2008
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Hamed Aissaoui, Martine Clozel, Walter Fischli, Ralf Koberstein, Thierry Sifferlen, Thomas Weller
  • Patent number: 7422837
    Abstract: A photosensitive composition comprising (i) at least one titanocene compound, (ii) a pyridine compound having a structure represented by formula (1) defined in the specification or a cyan compound having a structure represented by formula (3) defined in the specification, and (iii) a compound capable of undergoing a reaction with at least one of a radical and an acid to irreversibly change its physical or chemical property.
    Type: Grant
    Filed: February 16, 2005
    Date of Patent: September 9, 2008
    Assignee: FUJIFILM Corporation
    Inventor: Akinori Shibuya
  • Patent number: 7414132
    Abstract: A compound of the formula (I); wherein the variables X1 to X10, R1 to R7 including R3?, E, W, v, y, z, A and B are as described, or a pharmaceutically acceptable salt, solvate, enantiomer, racemate, diastereomer or mixtures thereof, useful for the treatment, prevention or amelioration of obesity and Related Diseases is disclosed.
    Type: Grant
    Filed: December 15, 2004
    Date of Patent: August 19, 2008
    Assignee: Eli Lilly and Company
    Inventors: Marta Garcia De La Torre, Nuria Diaz Buezo, Prabhakar Kondaji Jadhav, Charles Howard Mitch, Concepcion Pedregal-Tercero
  • Patent number: 7402671
    Abstract: Novel energy transfer dyes which can be used with shorter wavelength light sources are provided. These dyes include a donor dye with an absorption maxima at a wavelength between about 250 to 450 nm and an acceptor dye which is capable of absorbing energy emitted from the donor dye. One of the energy transfer dyes has a donor dye which is a member of a class of dyes having a coumarin or pyrene ring structure and an acceptor dye which is capable of absorbing energy emitted from the donor dye, wherein the donor dye has an absorption maxima between about 250 and 450 nm and the acceptor dye has an emission maxima at a wavelength greater than about 500 nm.
    Type: Grant
    Filed: March 10, 2006
    Date of Patent: July 22, 2008
    Assignee: Applera Corporation
    Inventor: Linda G. Lee
  • Publication number: 20080146801
    Abstract: A method of processing a substrate, including a step of processing an organic film pattern formed on a substrate, the step including, in sequence, a removal step of removing one of an alterated layer and a deposited layer formed on the organic film pattern, and a fusion/deformation step of fusing the organic film pattern for deformation, wherein at least a part of the removal step is carried out by applying chemical to the organic film pattern.
    Type: Application
    Filed: February 19, 2008
    Publication date: June 19, 2008
    Applicant: NEC LCD TECHNOLOGIES, LTD.
    Inventor: Shusaku KIDO
  • Patent number: 7384388
    Abstract: A combinatorial library of solid-state fluorescent dyes is prepared by reacting an aldehyde with a solid-supported pyridinium salt having a linker.
    Type: Grant
    Filed: April 13, 2005
    Date of Patent: June 10, 2008
    Assignee: New York University
    Inventor: Young-Tae Chang
  • Patent number: 7371769
    Abstract: The present invention relates to a group of novel tetrahydropyridin-4-yl indoles with a dual mode of action: serotonin reuptake inhibition and affinity for dopamine-D2 receptors, to methods for the preparation of these compounds and to novel intermediates useful for the synthesis of said tetrahydropyridin-4-yl indoles. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. The invention relates to novel tetrahydropyridin-4-yl indoles of the formula.
    Type: Grant
    Filed: December 6, 2005
    Date of Patent: May 13, 2008
    Assignee: Solvay Pharmaceuticals B.V.
    Inventors: Roelof van Hes, Pieter Smid, Cornelis G. Kruse, Martinus Th. M. Tulp
  • Patent number: 7351826
    Abstract: The invention provides compounds of Formula (I) that bind to GABAA receptors. In the above formula, variables are defined herein. Such compounds may be used to modulate ligand binding to GABAA receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) disorders in humans, domesticated companion animals, and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent(s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting GABAA receptors (e.g.
    Type: Grant
    Filed: February 16, 2004
    Date of Patent: April 1, 2008
    Assignee: Neurogen Corporation
    Inventors: Linghong Xie, Bingsong Han, Yuelian Xu
  • Patent number: 7348440
    Abstract: The present invention relates to dihydropyrrole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
    Type: Grant
    Filed: June 12, 2003
    Date of Patent: March 25, 2008
    Assignee: Merck & Co., Inc.
    Inventors: Kenneth L. Arrington, Paul J. Coleman, Christopher D. Cox, Mark E. Fraley, Robert M. Garbaccio, George D. Hartman, William F. Hoffman, Edward S. Tasber
  • Patent number: 7326723
    Abstract: The present invention relates to compounds of formula (I): in which X represents N or CH; R1 represents a hydrogen or halogen atom or a CF3 group; n is an integer from 1 to 5; A represents a partially saturated carbonaceous bi- or tricycle; it also relates to their salts, solvates, N-oxides, the pharmaceutical compositions containing them, a method for their preparation and synthesis intermediates in this method.
    Type: Grant
    Filed: October 14, 2002
    Date of Patent: February 5, 2008
    Assignee: Sanofi-Aventis
    Inventors: Marco Baroni, Bernard Bourrie, Rosanna Cardamone, Pierre Casellas
  • Patent number: 7301028
    Abstract: The present invention relates to dihydropyrazole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
    Type: Grant
    Filed: June 12, 2003
    Date of Patent: November 27, 2007
    Assignee: Merck & Co., Inc.
    Inventors: Kenneth L. Arrington, Mark E. Fraley
  • Patent number: 7279578
    Abstract: The invention relates to novel sulfonylamino-acetic acid derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of such compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as orexin receptor antagonists.
    Type: Grant
    Filed: October 6, 2003
    Date of Patent: October 9, 2007
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Hamed Aissaoui, Martine Clozel, Walter Fischli, Ralf Koberstein, Thierry Sifferlen, Thomas Weller
  • Patent number: 7276464
    Abstract: Catalysts useful for epoxidizing olefins are disclosed. The catalysts comprise a vinylpyridine polymer and a titanium zeolite. Preferably, the vinylpyridine polymer encapsulates the titanium zeolite. The catalysts are easy to prepare and use, they are easy to recover and reuse, and they convert olefins to epoxides in good yields with high selectivity. Surprisingly, ring-opening reactions that form glycol or glycol ether by-products are minimized by using the vinylpyridine polymer-containing catalysts. The catalysts are valuable for making propylene oxide from propylene and hydrogen peroxide. Vinylpyridine polymer-encapsulated transition metals and their use to produce hydrogen peroxide from hydrogen and oxygen is also disclosed.
    Type: Grant
    Filed: June 17, 2004
    Date of Patent: October 2, 2007
    Assignee: Lyondell Chemical Technology, L.P.
    Inventor: Bi Le-Khac
  • Patent number: 7273938
    Abstract: This invention relates to a new process for the preparation of novel substituted haloarene compounds of the formula I or IV: respectively, wherein R1, R2, R3, R4, R5, X, and Y are as defined herein, that comprises a novel and efficient selective mono-lithiation of a dihaloarene of the formula II or V: respectively, by an organo-lithium compound in the presence of a carbonyl reactant of the formula III: wherein R1 and R2 are as defined herein. In the process of the instant invention, the newly formed lithiated haloarene is sequentially quenched in situ by the carbonyl reactant to form said substituted haloarene. The process is suitable for batch or continuous flow systems.
    Type: Grant
    Filed: July 13, 2005
    Date of Patent: September 25, 2007
    Assignee: Pfizer Inc.
    Inventors: Jennifer L. Rutherford, Joel M. Hawkins
  • Patent number: 7256186
    Abstract: This invention discloses novel gamma secretase inhibitors of the formula: wherein: R1 is a substituted aryl or substituted heteroaryl group; R2 is an R1 group, alkyl, —XC(O)Y, alkylene-XC(O)Y, cycloalkylene-X—C(O)—Y, —CH—X—C(O)—NR3—Y or —CH—X—C(O)—Y, wherein X and Y are as defined herein; each R3 and each R3A are independently H, or alkyl; R11 is aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, or alkoxyalkyl. Also disclosed is a method of treating Alzheimer's Disease using one or more compounds of the invention.
    Type: Grant
    Filed: September 15, 2004
    Date of Patent: August 14, 2007
    Assignee: Schering Corporation
    Inventors: Dimitri A. Pissarntiski, Hubert B. Josien, Elizabeth M. Smith, John W. Clader, Theodros Asberom, Tao Guo, Douglas W. Hobbs
  • Publication number: 20070167626
    Abstract: An organic light emitting device having a pyrene based electron transport compound and an electron injecting and transport layer comprising the electron transport compound is provided.
    Type: Application
    Filed: January 16, 2007
    Publication date: July 19, 2007
    Inventors: Jung Keun Kim, Jeongdae Seo, Hyun Cheol Jeong, Jong Kwan Bin, Chungun Park
  • Patent number: 7220856
    Abstract: The present invention relates to CCR5 receptor antagonists of formulae (1a) or (1b): enantiomers, diastereomers, salts and solvates thereof wherein R1, R2, R3, R4, R5, and R7 are as defined herein. The invention further includes a method of CCR5-mediated disorders employing such compounds.
    Type: Grant
    Filed: June 26, 2003
    Date of Patent: May 22, 2007
    Assignee: Schering Aktiengesellschaft
    Inventors: Laura Dunning, Stefan Jaroch, Monica J. Kochanny, Wheeseong Lee, Xiongdong Lian, Meina Liang, Shou-Fu Lu, James Onuffer, Gary Phillips, Guo-Ping Wei, Bin Ye
  • Patent number: 7208602
    Abstract: This invention discloses novel gamma secretase inhibitors of the formula: wherein: R1 is a substituted aryl or substituted heteroaryl group; R2 is an R1 group, alkyl, —X(CO)Y, or alkylene-X(CO)Y wherein X and Y are as defined herein; each R3 and each R3A are independently H, or alkyl; R11 is aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, or alkoxyalkyl. Also disclosed is a method of treating Alzheimer's Disease using one or more compounds of the invention.
    Type: Grant
    Filed: February 5, 2003
    Date of Patent: April 24, 2007
    Assignees: Schering Corporation, Pharacopeia Drug Discovery, Inc.
    Inventors: Dmitri A. Pissarnitski, Hubert B. Josien, Elizabeth M. Smith, John W. Clader, Theodros Asberom, Tao Guo, Douglas W. Hobbs
  • Patent number: 7196111
    Abstract: The invention relates to the inhibition of hepatitis C virus (HCV) replication. In particular, embodiments of the invention provide compounds and methods for inhibiting HCV RNA-dependent RNA polymerase enzymatic activity. The invention also provides compositions and methods for the prophylaxis and treatment of HCV infection.
    Type: Grant
    Filed: June 2, 2003
    Date of Patent: March 27, 2007
    Assignee: Schering Corporation
    Inventors: Gerald W. Shipps, Kristin E. Rosner, Janet Popovici-Muller, Yongqi Deng, Tong Wang, Patrick J. Curran
  • Patent number: 7186834
    Abstract: The invention relates to novel substituted iminoazines of the general formula (I) in which R1, R2, R3, R4, Z1, Z2 and Z3 are each as defined in the disclosure, to a plurality of processes for their preparation, and to their use as herbicides.
    Type: Grant
    Filed: May 8, 2001
    Date of Patent: March 6, 2007
    Assignee: Bayer Aktiengesellschaft
    Inventors: Klaus-Helmut Müller, Mark Wilhelm Drewes, Peter Dahmen, Dieter Feucht, Rolf Pontzen
  • Patent number: 7186835
    Abstract: The composition relates to amino-imine compounds used in the formation of 1,3-diimine copper complexes for deposition of copper films.
    Type: Grant
    Filed: December 20, 2004
    Date of Patent: March 6, 2007
    Assignee: E. I. duPont de Nemours and Company
    Inventors: Alexander Zak Bradley, Jeffery Scott Thompson, David Lincoln Thorn
  • Patent number: 7094896
    Abstract: Disclosed are novel diaminothiazoles that are selective inhibitors of Cdk4. These compounds and their pharmaceutically acceptable salts and esters are anti-proliferative agents useful in the treatment or control of solid tumors, in particular breast, colon, lung and prostate tumors. Also disclosed are pharmaceutical compositions containing these compounds as well as intermediates useful in the preparation of the compounds.
    Type: Grant
    Filed: October 14, 2003
    Date of Patent: August 22, 2006
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Qingjie Ding, Paul Gillespie, Kyungjin Kim, Warren William McComas, Agostino Perrotta
  • Patent number: 7087755
    Abstract: A class of 2,4-; 2,3,4-; 2,4,6-; 2,3,4,5,6-substituted pyridines is provided which include novel compounds. The substitutions are achieved according to methods disclosed herein in which a metallated pyridine is reacted with an electrophile. Suitable electrophiles include CO2, SO2, dialkylcarbonates, ureas, formamides, amides, carboxylic acid esters, mono- and dihaloalkyls, halogens such as chlorine, fluorine, bromine, and iodine, metallic salts, sulfones, sulfonyls, aldehydes, ketones, anhydrides, nitrites, and electrophilic boron compounds including, but not limited to, boron trialkoxides and boron trihalides.
    Type: Grant
    Filed: November 10, 2005
    Date of Patent: August 8, 2006
    Assignee: Frontier Scientific, Inc.
    Inventors: Dustin R. Cefalo, Jason I. Henderson, Homayoun H. Mokri
  • Patent number: 7084250
    Abstract: The present invention relates to a process for the preparation of acetyl-amidiniophenylalanyl-cyclohexylglycyl-pyridinioalaninamides of the formula I, in which the anions X are physiologically acceptable anions, and their analogs, which are effective inhibitors of the blood coagulation factor Xa and which can be used, for example, for preventing thromboses. The process according to the invention comprises the coupling of 2-[2-acetylamino-3-(4-amidinophenyl)propionylamino]-2-cyclohexylacetic acid, which is obtained from 2-[2-acetylamino-3-(4-cyanophenyl)acryloylamino]-2-cyclohexylacetic acid by asymmetric hydrogenation and conversion of the cyano group into the amidine, or a salt thereof, with a 3-(2-amino-2-carbamoylethyl)-1-methylpyridinium salt or a salt thereof. The invention furthermore provides starting materials and intermediates for this process, processes for their preparation and acetyl-(S)-4-amidiniophenylalanyl-(S)-cyclohexylglycyl-(S)-(1-methyl-3-pyridinio)alaninamide as ditosylate salt.
    Type: Grant
    Filed: June 17, 2004
    Date of Patent: August 1, 2006
    Assignee: Sanofi-Aventis Deutschland GmbH
    Inventors: Gerhard Breipohl, Wolfgang Holla, Heiner Jendralla, Gerhard Beck
  • Patent number: 7083655
    Abstract: The present invention is directed to a hair dyeing composition comprising at least one azo dye of the following general formula (1): A—N=N—B??(1) where A=monovalent, optionally substituted heterocyclic group binding via the carbon atom to the azo group, that does not contain carboxy (—CO2H) or sulfo groups (SO3H) or quaternary ammonium groups and B=heterocyclic, aromatic or alkyl group containing a dissociative proton and, which is free of carboxy (—CO2H) or sulfo groups (—SO3H) or quaternary ammonium groups. Additionally, the present invention describes a method of dyeing human or animal hair by using such a dye and the use of this direct azo dye for dyeing human or animal hair. The use of this direct azo dye can impart the hair with an extremely vivid colour and has a less colour fade over the time.
    Type: Grant
    Filed: May 28, 2003
    Date of Patent: August 1, 2006
    Assignees: Kao Corporation, Fuji Photo Film Co., Ltd.
    Inventors: Dominic Pratt, Toshio Kawagishi
  • Patent number: 7078403
    Abstract: Disclosed herein are compounds of formula II: wherein Alk, Z, X1, X2, R1, —R10 and R11 are defined herein, and their salts and pharmaceutically acceptable derivatives thereof, as well as other compounds of the general formula Het-A-Alk-W-Ar-C(X2)?NO-X2 where Het, A, W and Ar are also defined herein. These compounds are useful in treating picornavirus infections in mammals. Novel intermediates of these compounds, as well as pharmaceutical compositions and methods of use, are also disclosed herein.
    Type: Grant
    Filed: June 16, 2000
    Date of Patent: July 18, 2006
    Assignee: Biota Scientific Management Pty Ltd.
    Inventors: Wen-Yang Wu, Keith Watson, Darryl McConnell, Betty Jin, Guy Krippner
  • Patent number: 7056355
    Abstract: The present invention is directed to a hair dyeing composition containing a dissociative azo dye of the following general formula (1) A-N?N—B??(1) wherein “A” represents a phenyl or naphthyl group which may be substitued; “B” represents an atomic group containing a dissociative proton, with the proviso “A” and “B” are free of sulfo, carboxyl and quaternary ammonium groups. Additionally, the present invention describes a method of dyeing human or animal hair by using such a dye and the use of this direct azo dye for dyeing human or animal hair. The use of this direct azo dye can impart the hair with an extremely vivid color and has less color fading over time.
    Type: Grant
    Filed: September 15, 2003
    Date of Patent: June 6, 2006
    Assignees: Kao Corporation, Fuji Photo Film Co., Ltd.
    Inventors: Dominic Pratt, Toshio Kawagishi
  • Patent number: 7045636
    Abstract: The present invention discloses compounds, which are novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.
    Type: Grant
    Filed: October 23, 2002
    Date of Patent: May 16, 2006
    Assignee: Schering Corporation
    Inventors: Anandan Palani, Sherry A. Shapiro, Mark D. McBriar, Jing Su
  • Patent number: 7018840
    Abstract: The present invention is directed, in part, to fluorescent metal sensors for detecting metal ions, and methods of making and using the same.
    Type: Grant
    Filed: April 17, 2002
    Date of Patent: March 28, 2006
    Assignee: Massachusetts Institute of Technology
    Inventors: Stephen J. Lippard, Shawn Burdette