Additional Hetero Ring Attached Directly Or Indirectly To The Diazole Ring By Nonionic Bonding (e.g., 1,3-dioxolan-2-yl Methyl-imidazole, Etc.) Patents (Class 548/311.1)
  • Patent number: 7407977
    Abstract: There are presented compounds of the formula or a pharmaceutically acceptable salt thereof, which are useful in the treatment of diabetes, diabetic retinopathy, asthma and diarrhea.
    Type: Grant
    Filed: July 29, 2005
    Date of Patent: August 5, 2008
    Assignee: Hoffman-La Roche Inc.
    Inventors: Jianping Cai, Adrian Wai-Hing, Fariborz Firooznia, Kevin Richard Guertin, Lida Qi
  • Patent number: 7399868
    Abstract: Compounds of Formula 1 where the variables have the meaning defined in the specification are agonists of alpha2 adrenergic receptors. Several compounds of the disclosure are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors. Additionally some of the claimed compounds have no or only minimal cardivascular and/or sedatory activity. The compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2 adrenergic receptors. Compounds of Formula 1 which have no significant cardiovascular and/or sedatory activity are useful for treating pain and other conditions with minimal side effects.
    Type: Grant
    Filed: September 20, 2005
    Date of Patent: July 15, 2008
    Assignee: Allergan, Inc.
    Inventors: Todd M. Heidelbaugh, Ken Chow, Phong X. Nguyen, Daniel W. Gil, John E. Donello, Michael E. Garst, Larry A. Wheeler
  • Patent number: 7378433
    Abstract: The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R1 is hydrogen, hydroxy, C1-6alkyl or aryl; R2 is hydrogen; optionally substituted C1-12alkyl; C3-7cycloalkyl; C2-8alkenyl, optionally substituted pyrrolidinyl or aryl; R3 is hydrogen, optionally substituted C1-6alkyl or aryl; Het is an optionally substituted unsaturated heterocycle selected from imidazolyl, triazolyl, tetrazolyl and pyridinyl; is an optionally substituted unsaturated mono- or bicyclic heterocycle; and aryl is optionally substituted phenyl. The present invention also relates to processes for their preparation and compositions comprising said new compounds, as well as their use as a medicine.
    Type: Grant
    Filed: December 13, 2006
    Date of Patent: May 27, 2008
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Marc Gaston Venet, Dominique Jean-Pierre Mabire, Jean Fernand Armand Lacrampe, Gerard Charles Sanz
  • Publication number: 20080119458
    Abstract: The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the histamine-3 receptor: wherein the variables are described in the specification.
    Type: Application
    Filed: October 5, 2007
    Publication date: May 22, 2008
    Applicant: Wyeth
    Inventors: William Ronald Solvibile, Ji-ln Kim, Marla Jean Williams, Jonathan Laird Gross, Albert Jean Robichaud
  • Patent number: 7368579
    Abstract: The present invention relates to a 1-substituted-4-nitroimidazole compound represented by the general formula (1) or a salt thereof, (wherein R is a hydrogen atom, a lower alkoxy group-substituted lower alkyl group, a phenyl-lower alkoxy group-substituted lower alkyl group, a cyano-substituted lower alkyl group, a phenyl-lower alkyl group which may have lower alkoxy groups as the substituents in the phenyl ring or a group of the formula —CH2RA; X is a halogen atom or a group of the formula —S(O)n—R1) and method for preparing the same. The compound of the formula (1) is a useful compound as an intermediate for synthesis of various pharmaceutical and agricultural chemicals, particularly, as intermediates for antitubercular agents.
    Type: Grant
    Filed: October 14, 2003
    Date of Patent: May 6, 2008
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Fumitaka Goto, Noriaki Takemura, Tadaaki Otani, Takeshi Hasegawa, Hidetsugu Tsubouchi, Naoto Utsumi, Shigekazu Fujita, Hideaki Kuroda, Takuya Shitsuta, Hirofumi Sasaki
  • Patent number: 7365210
    Abstract: The invention relates to a process for preparing chiral imidazolidin-2-ones of the formula I in which R1 is C1-C8-alkyl, cyclohexyl, phenyl, a C1-C6-alkyl-, halo-, nitro-, C1-C6-alkoxy-, C1-C6-alkylmercapto- or CF3-substituted phenyl radical, naphthyl or a C1-C6-alkyl-, halo-, nitro-, C1-C6-alkoxy- or CF3-substituted naphthyl radical, R2 is C1-C8-alkyl, C2-C8-alkenyl, cyclohexyl, phenyl or a phenyl-C1-C6-alkyl radical which may be substituted by a nitro, C1-C6-alkoxy, methylenedioxy or CF3 radical, and R3 is C1-C12-alkyl, C2-C8-alkenyl, cyclohexyl, phenyl or a C1-C6-alkyl-, halo-, nitro-, C1-C6-alkoxy-, methylenedioxy-, dialkylamino- or CF3-substituted phenyl radical, by reacting a compound of the formula II or the salt thereof in which R1, R2 and R3 have the abovementioned meaning, with urea in the presence of an involatile ammonium salt, wherein the reaction is carried out in the presence of an aprotic polar organic solvent.
    Type: Grant
    Filed: April 8, 2003
    Date of Patent: April 29, 2008
    Assignee: BASF Aktiengesellschaft
    Inventors: Hansgeorg Ernst, Jürgen Koppenhöfer, Daniela Klein
  • Publication number: 20080076932
    Abstract: A process for the preparation of olmesartan medoxomil, and derivatives thereof, by use of novel phenyltetrazole intermediates.
    Type: Application
    Filed: September 26, 2007
    Publication date: March 27, 2008
    Applicant: DIPHARMA FRANCIS S.R.L.
    Inventors: Gabriele RAZZETTI, Lino COLOMBO, Paola ROTA, Pietro ALLEGRINI
  • Patent number: 7338976
    Abstract: This invention relates to pharmaceutical compositions and methods for treating a vision disorder, improving vision, treating memory impairment, or enhancing memory performance using heterocyclic esters and amides.
    Type: Grant
    Filed: August 14, 1998
    Date of Patent: March 4, 2008
    Assignee: GPI NIL Holdings, Inc.
    Inventors: Douglas T. Ross, Gregory S. Hamilton, Joseph P. Steiner
  • Publication number: 20080045556
    Abstract: Compounds of the following structure are described: wherein R1, R2, R5, R6, V, X, Y, Z and Q are described herein, or a pharmaceutically acceptable salt, tautomer, metabolite or prodrug thereof. These compounds are useful for treating a variety of hormone-related conditions including contraception, treating or preventing fibroids, endometriosis, dysfunctional bleeding, uterine leiomyomata, polycystic ovary syndrome, or hormone-dependent carcinomas, providing hormone replacement therapy, stimulating food intake or synchronizing estrus.
    Type: Application
    Filed: August 13, 2007
    Publication date: February 21, 2008
    Applicant: Wyeth
    Inventors: Thomas Joseph Commons, Andrew Fensome, Gavin David Heffernan, Casey Cameron McComas, Richard Page Woodworth, Michael Byron Webb, Michael Anthony Marella, Edward George Melenski, Ronald Charles Bernotas
  • Publication number: 20080032994
    Abstract: The present invention relates to the compounds of formula (I), their preparation and use as antifungal and/or antibacterial agents. where the values for R1, R2, R3, R4, R5 and A are as defined herein.
    Type: Application
    Filed: November 2, 2006
    Publication date: February 7, 2008
    Inventors: Marcel Borgers, Maarten van Geffen, Jannie Ausma
  • Patent number: 7323433
    Abstract: The invention relates to R-(?)-1-[2-(7-Chloro-benzo[b]thiophen-3-yl-methoxy)-2-(2,4-dichloro-phenyl)-ethyl]-1H-imidazole and the salts thereof. The invention also relates to compositions thereof and their use either for treating fungal infections in humans and animals or combating crop diseases. A process for their preparation is also described.
    Type: Grant
    Filed: August 5, 2004
    Date of Patent: January 29, 2008
    Assignee: Ferrer Internacional, S.A.
    Inventors: Rafael Foguet, Jorge Ramentol, Lluis Anglada, Celia Palacin, Antonio Guglietta
  • Publication number: 20080015232
    Abstract: Methods and intermediates for preparing enantiomerically enriched Schweinfurthin analogs which are useful for the treatment of cancer, as well as novel Schweinfurthin analogs having anti-cancer activity, compositions comprising such analogs and therapeutic methods comprising administering such analogs.
    Type: Application
    Filed: March 29, 2005
    Publication date: January 17, 2008
    Inventors: David F. Wiemer, Jeffrey D. Neighbors, John A. Beutler
  • Patent number: 7304083
    Abstract: A 2-iminoimidazole derivative represented by the formula: {wherein R1, R2 and R3 represent hydrogen, optionally substituted C1-6 alkyl, etc.; R6 represents hydrogen, C1-6 alkyl, C1-6 alkyloxycarbonyl, etc.; Y1 represents a single bond, —CH2—, etc.; Y2 represents a single bond, —CO—, etc.; and Ar represents hydrogen, a group represented by the formula: [wherein R10–R14 represent hydrogen, C1-6 alkyl, hydroxyl, C1-6 alkoxy, etc., and R11 and R12 or R12 and R13 may bond together to form a 5- to 8-membered heterocycle], etc.}or salt thereof.
    Type: Grant
    Filed: April 19, 2002
    Date of Patent: December 4, 2007
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Shuichi Suzuki, Makoto Kotake, Mitsuaki Miyamoto, Tetsuya Kawahara, Akiharu Kajiwara, Ieharu Hishinuma, Kazuo Okano, Syuhei Miyazawa, Richard Clark, Fumihiro Ozaki, Nobuaki Sato, Masanobu Shinoda, Atsushi Kamada, Itaru Tsukada, Fumiyoshi Matsuura, Yoshimitsu Naoe, Taro Terauchi, Yoshiaki Oohashi, Osamu Ito, Hiroshi Tanaka, Takashi Musha, Motoji Kogushi, Tsutomu Kawata, Toshiyuki Matsuoka, Hiroko Kobayashi, Ken-ichi Chiba, Akifumi Kimura, Naoto Ono
  • Publication number: 20070259924
    Abstract: The present invention is directed to compounds of formula (I) and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to intermediates used in making such compounds, pharmaceutical compositions containing such a compound, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.
    Type: Application
    Filed: May 4, 2007
    Publication date: November 8, 2007
    Inventors: Yonghong Song, Zhaozhong J. Jia, Anjali Pandey, Robert M. Scarborough, Carroll Scarborough
  • Patent number: 7291642
    Abstract: The present invention provides bradykinin-B1 antagonists of the formula in which A, Ar, G, Q, R1 and R4 are as defined in claim 1, their enantiomers, their diastereomers, their mixtures and their salts, in particular their physiologically acceptable salts with organic or inorganic acids or bases having useful properties, their preparation, medicaments comprising the pharmacologically effective compounds, their preparation and their use.
    Type: Grant
    Filed: October 21, 2005
    Date of Patent: November 6, 2007
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Iris Kauffmann-Hefner, Norbert Hauel, Henri Doods, Angelo Ceci, Stefan Peters
  • Publication number: 20070249680
    Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.
    Type: Application
    Filed: April 18, 2007
    Publication date: October 25, 2007
    Inventors: Carl R. Illig, Shelley K. Ballentine, Jinsheng Chen, Renee Louise DesJarlais, Sanath K. Meegalla, Bruce E. Tomczuk, Mark Wall, Kenneth Wilson
  • Publication number: 20070249685
    Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.
    Type: Application
    Filed: April 18, 2007
    Publication date: October 25, 2007
    Inventors: Carl R. Illig, Jinsheng Chen, Renee Louise DesJarlais, Kenneth Wilson
  • Patent number: 7279497
    Abstract: The present invention relates to benzopyran derivatives substituted with secondary amines including imidazole, their preparation, and pharmaceutical compositions containing them. The present invention is pharmacologically useful for the treatment of cancer, rheumatoid arthritis, and diabetic retinopathies through anti-angiogenic properties, and also pharmacologically useful in the protection of heart and neuronal cells against ischemia-reperfusion injury or preserving organs.
    Type: Grant
    Filed: July 30, 2003
    Date of Patent: October 9, 2007
    Assignee: Korea Research Institute of Chemical Technology
    Inventors: Kyu Yang Yi, Sun Kyung Lee, Sung-Eun Yoo, Jee Hee Suh, Nak Jeong Kim, Sun Kyung Hwang, Byung-Ho Lee, Ho Won Seo, Chong Ock Lee, Sang-Un Choi
  • Patent number: 7271270
    Abstract: This invention relates to low molecular weight, non-peptidic, non-peptidomimetic, organic molecules that act as modulators of mammalian complement C5a receptors, preferably ones that act as high affinity C5a receptor ligands and also to such ligands that act as antagonists or inverse agonists of complement C5a receptors. Preferred compounds of the invention possess some or all of the following properties in that they are: 1) multi-aryl in structure, 2) heteroaryl in structure, 3) a pharmaceutically acceptable oral dose can provide a detectable in vitro effect, 4) comprise fewer than four or preferably no amide bonds, and 5) capable of inhibiting leukocyte chemotaxis at nanomolar or sub-nanomolar concentrations. This invention also relates to pharmaceutical compositions comprising such compounds and the use of such compounds in treating a variety of inflammatory and immune system disorders. Additionally, this invention relates to the use such compounds as probes for the localization of C5a receptors.
    Type: Grant
    Filed: May 24, 2004
    Date of Patent: September 18, 2007
    Assignee: Neurogen Corporation
    Inventors: Andrew Thurkauf, Xiao-shu He, He Zhao
  • Patent number: 7265150
    Abstract: This invention relates to novel compositions and uses of N-heterocyclic carboxylic acids and carboxylic acid isosteres for treating a vision disorder, improving vision, treating memory impairment or enhancing memory performance in an animal.
    Type: Grant
    Filed: August 14, 1998
    Date of Patent: September 4, 2007
    Assignee: GPI NIL Holdings Inc.
    Inventors: Douglas T. Ross, Hansjörg Sauer, Gregory S. Hamilton, Joseph P. Steiner
  • Publication number: 20070197617
    Abstract: The present invention relates to compounds of the formula methods for the preparation thereof, and methods for their use. The compounds are useful in treating diseases characterized by the hyperactivity of MEK. Accordingly the compounds are useful in the treatment of diseases, such as cancer, cognitive and CNS disorders, and inflammatory/autoimmune diseases.
    Type: Application
    Filed: January 25, 2007
    Publication date: August 23, 2007
    Inventors: Shaoqing Chen, Nicholas J. S. Huby, Norman Kong, Steven Gregory Mischke, John Anthony Moliterni, Hong Wang, Zhuming Zhang
  • Patent number: 7259263
    Abstract: The invention relates to methods of synthesizing 2-substituted azole compunds of formula (I): The invention is also relates to compounds of formula (I) and to intermediate compounds in the synthesis method.
    Type: Grant
    Filed: June 29, 2005
    Date of Patent: August 21, 2007
    Assignee: Jansen Pharmaceutica N.V.
    Inventors: Dennis J. Hlasta, Craig A. Zificsak
  • Publication number: 20070191313
    Abstract: 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: Application
    Filed: February 15, 2007
    Publication date: August 16, 2007
    Inventors: Richard L. Beard, John E. Donello, Haiqing Yuan, Diana F. Colon, Tien Duong, Xiaoxia Liu, Yihui Hu
  • Patent number: 7253200
    Abstract: Imidazole compounds, compositions, and methods of using them in leukocyte recruitment inhibition, in modulating H4 receptor expression, and in treating conditions such as inflammation, H4 receptor-mediated conditions, and related conditions.
    Type: Grant
    Filed: March 24, 2005
    Date of Patent: August 7, 2007
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Daniel J. Buzard, James P. Edwards, David E. Kindrachuk, Jennifer D. Venable
  • Patent number: 7253199
    Abstract: The invention provides substituted pyrazolidinone compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are useful for a variety of therapies, including treating or preventing various cancers, inflammation, septic shock, preterm labor, infertility, pain, and ischemia, and other diseases and disorders associated with MEK-1 and/or ERK-2 activation.
    Type: Grant
    Filed: October 23, 2002
    Date of Patent: August 7, 2007
    Assignee: Applied Research Systems ARS Holding N.V.
    Inventors: Stephen J. Arkinstall, Antonio Arulanandam, Xuliang Jiang, Sharad Magar, Roustem Nabioullin, John Yingsheng Zhang, Peter Blume-Jensen
  • Patent number: 7244739
    Abstract: Novel compounds, compositions, and kits are provided. Methods of modulating A? levels, and methods of treating a disease associated with aberrant A? levels are also provided.
    Type: Grant
    Filed: May 14, 2004
    Date of Patent: July 17, 2007
    Assignee: Torreypines Therapeutics, Inc.
    Inventors: Soan Cheng, Daniel D. Comer, Long Mao, Guity P. Balow, David Pleynet
  • Patent number: 7241787
    Abstract: The invention relates to substituted N-cyclohexylheterocycles and to the physiologically tolerated salts and physiologically functional derivatives thereof, to processes for their preparation and to their use as medicaments. Compounds of the formula I, in which the radicals have the stated meanings, and the physiologically tolerated salts thereof, and process for their preparation are described. The compounds bring about for example a weight reduction in mammals and are suitable for example for the prevention and treatment of obesity and diabetes.
    Type: Grant
    Filed: January 25, 2005
    Date of Patent: July 10, 2007
    Assignee: Sanofi-Aventis Deutschland GmbH
    Inventors: Lothar Schwink, Thomas Boehme, Matthias Gossel, Siegfried Stengelin
  • Patent number: 7230114
    Abstract: Compounds of formula (I), methods for their preparation and their use in the manufacture of neuraminidase inhibitor conjugates.
    Type: Grant
    Filed: August 30, 2002
    Date of Patent: June 12, 2007
    Assignee: Biota Scientific Management Pty Ltd
    Inventors: Brian David Judkins, Simon John Fawcett MacDonald, Derek Anthony Demaine, Graham George Adam Inglis, Julie Nicole Hamblin
  • Patent number: 7202263
    Abstract: N-Heterocyclic derivatives of the following formula: where m, n, p, A1, R1, R2, R3 and R4 are described herein, as well as other N-heterocyclic derivatives, are useful as inhibitors of nitric oxide synthase. Pharmaceutical compositions containing these compounds, methods of using these compounds as inhibitors of nitric oxide synthase and processes for synthesizing these compounds are also described herein.
    Type: Grant
    Filed: December 16, 2005
    Date of Patent: April 10, 2007
    Assignee: Schering Aktiengesellschaft
    Inventors: David Davey, Raju Mohan, Gary Phillips, Guo Ping Wei, Wei Xu
  • Patent number: 7196108
    Abstract: The invention relates to certain bicyclic heterocycles havng the structure shown below which are useful in the treatment of diseases related to lipid and carbohydrate metabolism, such as type 2 diabetes, and atherosclerosis.
    Type: Grant
    Filed: March 6, 2003
    Date of Patent: March 27, 2007
    Assignees: Incyte San Diego Inc., Ortho McNeil Pharmaceutical Inc.
    Inventors: Magnus Pfahl, Catherine Tachdjian, Hussien A. Al-Shamma, Andrea Fanjul Giachino, Karine Jakubowicz-Jaillardon, Jianhua Guo, Richard M. Fine, Lyle W. Spruce, James W. Zapf
  • Patent number: 7189755
    Abstract: Melanocortin receptor-specific pyrrolidine compounds having the structure: and stereoisomer and pharmaceutically acceptable salts thereof, where R1, R2, and R3 are as described in the specification, preferably where R3 is a D-amino acid with at least one substituted or unsubstituted phenyl or naphthyl aromatic ring, and where R3 optionally further includes an amine capping group or from one to three additional amino acid residues, optionally with an amine capping group, which compounds are agonists, antagonists or mixed agonists and antagonists at one or more melanocortin receptors, and having utility in the treatment of melanocortin receptor-related disorders and conditions. Methods of synthesis of compounds of structure (I), pharmaceutical compositions containing a compound of structure (I) and methods relating to the use thereof are also disclosed.
    Type: Grant
    Filed: February 10, 2004
    Date of Patent: March 13, 2007
    Assignee: Palatin Technologies, Inc.
    Inventors: Shubh D. Sharma, Yi-Qun Shi, Zhijun Wu, Ramesh Rajpurohit
  • Patent number: 7157476
    Abstract: The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
    Type: Grant
    Filed: August 20, 2004
    Date of Patent: January 2, 2007
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jon H. Come, Jeremy Green, Craig Marhefka, Scott L. Harbeson, Ly Pham
  • Patent number: 7129359
    Abstract: This invention relates to compounds of the following formula: in which R1, R2, A1, A2, X, Y, m, n, p, x and y are as defined herein, pharmaceutical compositions comprising the compounds and use of the compounds in treating enterovirus infection.
    Type: Grant
    Filed: November 19, 2003
    Date of Patent: October 31, 2006
    Assignee: National Health Research Institutes
    Inventors: Jyh-Haur Chern, Shin-Ru Shih, Chiung-Tong Chen, Chih-Shiang Chang, Chung-Chi Lee, Yen-Chun Lee, Chia-Liang Tai
  • Patent number: 7091221
    Abstract: According to the present invention, there are provided a novel partial ester of a nitrogenous carboxylic acid ester with cellulose, the partial ester being useful as an antibacterial agent, a flame retardant, etc., and a simple and convenient process for preparing the same. Fibers made of said partial ester have washing-resistant antibacterial property and flame retardancy. There can be prepared the partial ester of a nitrogenous carboxylic acid ester with cellulose by contacting a nitrogenous carboxylic acid ester with cellulose and heat-treating the mixture.
    Type: Grant
    Filed: December 19, 2000
    Date of Patent: August 15, 2006
    Assignee: Ajinomoto Co., Inc.
    Inventors: Masahiko Kurauchi, Kiyonori Furuta, Hiroyuki Sato
  • Patent number: 7049296
    Abstract: Urea derivatives of formula I are disclosed: The compounds are inhibitors of ?-secretase, and hence useful in the treatment or prevention of Alzheimer's Disease
    Type: Grant
    Filed: February 28, 2001
    Date of Patent: May 23, 2006
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Jose Luis Castro Pineiro, Adrian Leonard Smith, Graeme Irvine Stevenson
  • Patent number: 7045535
    Abstract: Certain cyclic compounds are presented as well as their use for inhibiting paramyxovirus neuraminidase.
    Type: Grant
    Filed: March 8, 2002
    Date of Patent: May 16, 2006
    Assignee: BioCryst Pharmaceuticals, Inc.
    Inventors: Pooran Chand, Yarlagadda S. Babu, R. Scott Rowland, Tsu-Hsing Lin
  • Patent number: 7041693
    Abstract: The present application describes novel hydantoin derivatives of formula (I): or pharmaceutically acceptable salt or prodrug forms thereof, wherein L, Z0, R1, R4, R5, and R11 are defined in the present specification, which are useful as inhibitors of matrix metalloproteinases (MMP), TNF-? converting enzyme (TACE), aggrecanase, or a combination thereof.
    Type: Grant
    Filed: October 2, 2003
    Date of Patent: May 9, 2006
    Assignee: Bristol-Myers Squibb Company
    Inventor: James Sheppeck
  • Patent number: 7022727
    Abstract: The present invention relates to a crystalline form of 6-[(2,2-diphenylethyl)amino]-9-(N-ethyl-?-D-ribofuranosyluronamide)-N-(2-{N?-[1-(2-pyridyl)-4-piperidyl]ureido}ethyl)-9H-purine-2-carboxamide and to a process for the preparation of, compositions containing and the uses of such a crystalline form.
    Type: Grant
    Filed: September 3, 2004
    Date of Patent: April 4, 2006
    Assignee: Pfizer Inc
    Inventors: Terence Vernon Silk, Julian Duncan Smith
  • Patent number: 7002019
    Abstract: A method of synthesizing aromatic ketone compositions of formula I comprising the step of introducing a double bond into the 5 membered ring of the 4,5-dihydro-1,3-azoles moiety of formula II is disclosed. A method of synthesizing aromatic ketone compositions of formula I comprising the step of ring synthesis of the tetrahydro-1,3-azoles of formula XI is also disclosed.
    Type: Grant
    Filed: February 11, 2003
    Date of Patent: February 21, 2006
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Pawel K. Grzywacz, Rafal R. Sicinski
  • Patent number: 6995182
    Abstract: The present invention is a series of compounds that are derivatives of 1-sulfonyl-pyrrolidine and that demonstrate affinity towards metabotropic glutamate receptors. The invention further relates to medicaments containing these compounds and to a process for their preparation. The compounds possess affinity towards metabotropic glutamate receptors and are therefore useful in the treatment or prevention of acute and/or chronic neurological disorders.
    Type: Grant
    Filed: March 26, 2003
    Date of Patent: February 7, 2006
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Vincent Mutel, Juergen Wichmann
  • Patent number: 6987104
    Abstract: N-[1-oxo-(optionally 2-aza)-2-alkyl-3-(carboxyl or thiol or hydroxyaminocarbonyl or N-hydroxyformamido)-propyl]-(aryl or heteroaryl)-azacyclo4-7alkanes or thiazacyclo4-7alkanes, salts or prodrugs thereof have interesting properties, e.g., in the treatment or prevention of disorders amenable to treatment by PDF inhibitors, such as treatment of bacterial infections.
    Type: Grant
    Filed: June 14, 2002
    Date of Patent: January 17, 2006
    Assignee: Vicuron Pharmaceuticals Inc.
    Inventors: Jeffrey Jacobs, Rakesh K. Jain, Jason G. Lewis, Dinesh V. Patel, Zhengyu Yuan
  • Patent number: 6949578
    Abstract: The present invention relates to a class of compounds represented by the Formula I or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the ?v?3 and/or ?v?5 integrin.
    Type: Grant
    Filed: July 14, 2004
    Date of Patent: September 27, 2005
    Assignee: Pharmacia Corporation
    Inventors: Ish Kumar Khanna, Michael Clare, Alan F. Gasiecki, Thomas Rogers, Barbara Chen, Mark Russell, Hwang-Fun Lu
  • Patent number: 6949538
    Abstract: Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.
    Type: Grant
    Filed: July 17, 2003
    Date of Patent: September 27, 2005
    Assignees: Cytokinetics, Inc., Smithkline Beecham Corporation
    Inventors: Andrew McDonald, Gustave Bergnes, David J. Morgans, Jr., Dashyant Dhanak, Steven David Knight
  • Patent number: 6936596
    Abstract: 2-(6-Cyano-1-hexyn-1-yl)adenosine, 2-(6-cyano-1-hexyn-1-yl)adenosine 5?-monophosphate, or salts thereof; and drugs containing the same as an active ingredient. The compounds have excellent effects of lowering ocular tension, promoting blood flow in retina, and protecting optic nerve failure and are highly soluble in water. Owing to these characteristics, the compounds are useful as drugs such as remedies for glaucoma and ocular hypertension.
    Type: Grant
    Filed: September 7, 2001
    Date of Patent: August 30, 2005
    Assignees: Toa Eiyo Ltd., Yamasa Corporation
    Inventors: Takashi Konno, Kazuhiro Uemoto, Shinya Onuma, Yoshikazu Kato
  • Patent number: 6900161
    Abstract: The invention concerns novel azole or triazole derivatives of formula (Ia) or (Ib), wherein: X, Ar1, Ar2, Ar3, A, B and R1 are such as defined in the description, the method for preparing same and their use as fungicides.
    Type: Grant
    Filed: January 9, 2004
    Date of Patent: May 31, 2005
    Assignee: Aventis Pharma S.A.
    Inventors: Didier Babin, John Bernard Weston
  • Patent number: 6884815
    Abstract: This invention relates to low molecular weight, non-peptidic, non-peptidomimetic, organic molecules that act as modulators of mammalian complement C5a receptors, preferably ones that act as high affinity C5a receptor ligands and also to such ligands that act as antagonists or inverse agonists of complement C5a receptors. Preferred compounds of the invention possess some or all of the following properties in that they are: 1) multi-aryl in structure, 2) heteroaryl in structure, 3) a pharmaceutically acceptable oral dose can provide a detectable in vitro effect, 4) comprise fewer than four or preferably no amide bonds, and 5) capable of inhibiting leukocyte chemotaxis at nanomolar or sub-nanomolar concentrations. This invention also relates to pharmaceutical compositions comprising such compounds and the use of such compounds in treating a variety of inflammatory and immune system disorders. Additionally, this invention relates to the use such compounds as probes for the localization of C5a receptors.
    Type: Grant
    Filed: June 12, 2003
    Date of Patent: April 26, 2005
    Assignee: Neurogen Corporation
    Inventors: Andrew Thurkauf, Xiao-shu He, He Zhao, John Peterson, Xiaoyan Zhang, Robbin Brodbeck, James Krause, George Maynard, Alan Hutchison
  • Patent number: 6867305
    Abstract: The present invention provides convergent processes for preparing epothilones, desoxyepothilones, and analogues thereof. The present invention further provides novel compositions and methods for the treatment of cancer and additionally provides methods for the treatment of cancer which has developed a multi-drug phenotype.
    Type: Grant
    Filed: March 1, 2001
    Date of Patent: March 15, 2005
    Assignee: Sloan-Kettering Institute for Cancer Research
    Inventors: Samuel J. Danishefsky, Shawn J. Stachel, Chul Bom Lee, Mark D. Chappell, Zhical Wu
  • Patent number: 6864270
    Abstract: Composition, article of manufacture for and method of treating malaria in a human having an infestation of Plasmodium protozoans are described. The method comprises administering a therapeutically-effective amount of a compound of formula (I) or (IV), i.e. sufficient quantity to reduce the population of Plasmodium. The composition of the invention is a compound of formula (I) or (IV) with a pharmaceutical excipient. The article of manufacture is the composition in combination with labeling for treating malaria. The substituents are detailed in the specification.
    Type: Grant
    Filed: August 8, 2002
    Date of Patent: March 8, 2005
    Assignee: University of Florida Research Foundation, Inc.
    Inventor: Raymond J. Bergeron, Jr.
  • Patent number: 6852746
    Abstract: The present invention relates to a crystalline form of 6-[(2,2-diphenylethyl)amino]-9-(N-ethyl-?-D-ribofuranosyluronamide)-N-(2-{N?-[1-(2-pyridyl)-4-piperidyl]ureido}ethyl)-9H-purine-2-carboxamide and to a process for the preparation of, compositions containing and the uses of such a crystalline form.
    Type: Grant
    Filed: December 3, 2002
    Date of Patent: February 8, 2005
    Assignee: Pfizer Inc
    Inventors: Terence Vernon Silk, Julian Duncan Smith
  • Publication number: 20040259884
    Abstract: The present invention provides compounds according to formula I 1
    Type: Application
    Filed: June 14, 2004
    Publication date: December 23, 2004
    Inventors: Gregory Jay Haley, Norman Kong, Emily Aijun Liu, Klaus B. Simonsen, Binh Thanh Vu, Stephen Evan Webber