Nitrogen Bonded Directly To The -c(=x)- Group Patents (Class 546/175)
  • Publication number: 20090084441
    Abstract: The invention relates to a photoelectric conversion device, using oxide semiconductor fine particles sensitized with a methine dye represented by the following formula (1) and a solar cell using the same, and a solar cell high in conversion efficiency can be obtained at low cost: in the formula (1), n represents an integer of 0 to 7; R1 represents an optionally-substituted aromatic residue or optionally-substituted aliphatic hydrocarbon residue, or an acyl group; X represents an optionally-substituted hydrocarbon residue which has 2 to 4 carbon atoms; Y represents a hydrogen atom, an optionally-substituted aromatic residue or aliphatic hydrocarbon residue, a carboxyl group or the like, and preferably represents a carboxyl group; Z represents an optionally-substituted aromatic residue or aliphatic hydrocarbon residue, or an acyl group; A1, A2 and A3 each independently represent a hydrogen atom, an optionally-substituted aromatic residue or aliphatic hydrocarbon residue or the like, and preferably represent
    Type: Application
    Filed: May 23, 2006
    Publication date: April 2, 2009
    Inventors: Koichiro Shigaki, Masayoshi Kaneko, Akira Maenosono, Takayuki Hoshi, Teruhisa Inoue
  • Publication number: 20090069321
    Abstract: The present invention relates to cyanomethyl substituted N-acyl tryptamines of the formula I in which R1, R2, R3, R4, R5, Q, X and W have the meaning as defined in the description. The compounds according to the invention are effective FSH antagonists and can be used for example for fertility control in men or in women, or for the prevention and/or treatment of osteoporosis.
    Type: Application
    Filed: July 29, 2008
    Publication date: March 12, 2009
    Inventors: Lars WORTMANN, Marcus Koppitz, Florian Peter Liesener, Thomas Frenzel, Hans-Peter Muhn, Anna Schrey, Ronald Kuehne
  • Publication number: 20090069316
    Abstract: The invention relates to compounds represented by Formula (I): and to pharmaceutically acceptable salts or solvates of said compounds, wherein each of A, R3-8, X3, X5, m, and n are defined herein. The invention also relates to pharmaceutical compositions containing the compounds of Formula (I) and to methods of treating hyperproliferative disorders in a mammal by administering compounds of Formula (I).
    Type: Application
    Filed: March 31, 2008
    Publication date: March 12, 2009
    Inventors: Yufeng Hong, Robert Steven Kania
  • Publication number: 20090054235
    Abstract: The present invention relates to novel benzoheterocyclylethylbenzamide derivatives of formula (I) in which the substituents are in the description, their process of preparation, their use as fungicides, particularly in the form of fungicidal compositions, and methods for the control of phytopathogenic fungi of plants using these compounds or their compositions.
    Type: Application
    Filed: July 6, 2006
    Publication date: February 26, 2009
    Inventors: Darren Mansfield, Pierre-Yves Coqueron, Heiko Rieck, Philippe Desbordes, Alain Villier, Marie-Claire Grosjean-Cournoyer, Pierre Genix
  • Publication number: 20090041721
    Abstract: The present invention discloses compounds of Formula I or II, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. 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 to the subject a pharmaceutical composition comprising a compound of the present invention.
    Type: Application
    Filed: August 9, 2007
    Publication date: February 12, 2009
    Inventors: Deqiang Niu, Yonghua Gai, Yat Sun Or, Zhe Wang
  • Publication number: 20090036436
    Abstract: Compounds of Formulas 1 and 2 where the variables have the meaning disclosed in the specification, have analgesic and in some cases immunostimulant activity.
    Type: Application
    Filed: January 25, 2006
    Publication date: February 5, 2009
    Inventors: Bertrand Leblond, Eric Beausoleil, Thierry Taverne, John E. Donello
  • Publication number: 20090028858
    Abstract: The present invention relates to new substituted quinoline compounds and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the new compounds together with pharmaceutically acceptable carriers, and uses of the new compounds.
    Type: Application
    Filed: September 30, 2008
    Publication date: January 29, 2009
    Inventors: Weibo Wang, Ryan N. Constantine, Liana Marie Lagniton, Kenneth Bair
  • Publication number: 20090023761
    Abstract: Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110? activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lympho
    Type: Application
    Filed: March 24, 2008
    Publication date: January 22, 2009
    Inventors: Yi Chen, Timothy D. Cushing, Xiaolin Hao, Xiao He, Andreas Reichelt, Robert M. Rzasa, Jennifer Seganish, Youngsook Shin, Dawei Zhang
  • Publication number: 20080318944
    Abstract: Disclosed are N-aroyl cyclic amine derivatives having the formula: where the variables are as define herein, and their use as pharmaceuticals, specifically as orexin receptor antagonists.
    Type: Application
    Filed: October 29, 2007
    Publication date: December 25, 2008
    Inventors: Clive Leslie BRANCH, Wai Ngor Chan, Amanda Johns, Christopher Norbert Johnson, David John Nash, Riccardo Novelli, Jean-Pierre Pilleux, Roderick Alan Porter, Rachel Elizabeth, Anne Stead, Geoffrey Stemp
  • Publication number: 20080287428
    Abstract: A compound represented by formula (I?): (wherein m, n, and p each represent 0 to 2; q represents 0 or 1; R1 represents halogen, a hydrocarbon group, a heterocyclic group, an alkoxy group, an alkoxycarbonyl group, a sulfamoyl group, a CN group, an NO2 group, or the like; R2 represents halogen, amino, a hydrocarbon group, an aromatic heterocyclic group, or an oxo group; X1 represents O, —NR3—, or —S(O)r-; X2 represents a methylene group, O, —NR3—, or —S(O)r-; Q? represents a heteroaryl group, a heteroarylalkyl group, a substituted aryl group, or an aralkyl group; Cycle moiety represents an aryl ring or a heteroaryl ring; and the wavy line represents an E-isomer or a Z-isomer), a salt of the compound, or a solvate of the compound or the salt. A pharmaceutical composition and a transient receptor potential type I (TRPV1) receptor antagonist each contain, as an active ingredient, at least one of the compound, a salt of the compound, and a solvate of the compound or the salt.
    Type: Application
    Filed: July 24, 2006
    Publication date: November 20, 2008
    Applicant: Mochida Pharmaceutical Co.,Ltd
    Inventors: Hideharu Uchida, Naoto Kosuga, Tsutomu Satoh, Daido Hotta, Tomoyuki Kamino, Yoshitaka Maeda, Ken-ichi Amano, Yasushige Akada
  • Publication number: 20080269265
    Abstract: This invention relates to the use of a group of aryl ureas in treating raf mediated diseases, and pharmaceutical compositions for use in such therapy.
    Type: Application
    Filed: June 25, 2008
    Publication date: October 30, 2008
    Inventors: Scott Miller, Martin Osterhout, Jacques Dumas, Uday Khire, Timothy B. Lowinger, Bernd Riedl, William J. Scott, Roger A. Smith, Jill E. Wood, David Gunn, Martha Rodriguez, Ming Wang, Tiffany Turner, Catherine Brennan
  • Publication number: 20080269213
    Abstract: The present invention relates to 8-Hydroxyquinoline Compounds; compositions comprising an 8-Hydroxyquinoline Compound; and methods for treating or preventing a metalloproteinase-related disorder, such as, an arthritic disorder, osteoarthritis, malignant neoplasm, rheumatoid arthritis, asthma, chronic obstructive pulmonary disease, atherosclerosis, age-related macular degeneration, myocardial infarction, a corneal ulceration, an ocular surface disease, hepatitis, an aortic aneurysm, tendonitis, a central nervous system disorder, abnormal wound healing, angiogenesis, restenosis, cirrhosis, multiple sclerosis, glomerulonephritis, graft versus host disease, diabetes, an inflammatory bowel disease, shock, invertebral disc degeneration, stroke, osteopenia or a periodontal disease or comprising administering an effective dose of an 8-Hydroxyquinoline Compound to a mammal in need thereof.
    Type: Application
    Filed: August 23, 2007
    Publication date: October 30, 2008
    Applicant: Wyeth
    Inventors: Matthew G. Bursavich, Sabrina Lombardi, Adam M. Gilbert, Leif Mark Laakso, Gulnaz Khafizova, David Brian How, Joshua James Sabatini, Phaik-Eng Sum, Jeremy Clemens
  • Publication number: 20080167468
    Abstract: The present invention relates to a diastereomeric mixture of Silacycle Compounds and methods for using the diastereomeric mixture of Silacycle Compounds for stereoselective synthesis.
    Type: Application
    Filed: June 6, 2007
    Publication date: July 10, 2008
    Applicant: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK
    Inventors: James Lincoln Leighton, Richard Berger, Seiji Shirakawa, Gregory T. Notte
  • Patent number: 7319148
    Abstract: The invention concerns novel nucleotide analogues comprising a reactive hydrazide function used as initial synthons for preparing compounds (formula I) capable of inducing mutations or capable of inhibiting a DNA polymerase or a kinase. The invention also concerns nucleic acids comprising said nucleotide and nucleoside analogues.
    Type: Grant
    Filed: June 13, 2001
    Date of Patent: January 15, 2008
    Assignee: Institut Pasteur
    Inventors: Philippe Marliere, Sylvie Pochet
  • Patent number: 7312234
    Abstract: Tertiary amines containing a multiplicity of heteroaromatic substituents are useful as chemokine receptor modulators.
    Type: Grant
    Filed: August 9, 2004
    Date of Patent: December 25, 2007
    Assignee: AnorMED
    Inventors: Gary Bridger, Renato Skerlj, Al Kaller, Curtis Harwig, David Bogucki, Trevor R. Wilson, Jason Crawford, Ernest J. McEachern, Bem Atsma, Siqiao Nan, Yuanxi Zhou, Dominique Schols, Christopher Dennis Smith, Maria Rosaria Di Fluri
  • Patent number: 7288559
    Abstract: The present invention is directed to compounds that are antagonists of CGRP receptors and that are useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. 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 CGRP is involved.
    Type: Grant
    Filed: March 10, 2004
    Date of Patent: October 30, 2007
    Assignee: Merck + Co, Inc.
    Inventors: Ian M. Bell, Steven N. Gallicchio, Craig A. Stump, C. Blair Zartman
  • Patent number: 7265115
    Abstract: Compounds of formula I: or pharmaceutically acceptable salts thereof, are useful for controlling synaptic transmission in mammals.
    Type: Grant
    Filed: April 11, 2003
    Date of Patent: September 4, 2007
    Assignee: Abbott Laboratories
    Inventors: William H. Bunnelle, Daniela Barlocco Cristina, Jerome F. Daanen, Michael J. Dart, Michael D. Meyer, Keith B. Ryther, Michael R. Schrimpf, Kevin B. Sippy, Richard B. Toupence
  • Patent number: 7241776
    Abstract: Novel cyanoamidines compounds of formula (I) and (II) and their derivatives wherein R1-R12 are as defined in the specification act as antagonists of the P2X7 receptor. These compounds are particularly useful in the treatment of pain, inflammation and neurodegeneration states.
    Type: Grant
    Filed: August 2, 2004
    Date of Patent: July 10, 2007
    Assignee: Abbott Laboratories
    Inventors: William A. Carroll, Arturo Perez-Medrano, Sridhar Peddi, Alan S. Florjancic
  • Patent number: 7151175
    Abstract: The invention refers to novel propenecarboxylic acid amidoxime derivatives furthermore N-oxides and/or geometrical isomers and/or optical isomers and/or pharmaceutically suitable acid addition salts and/or quaternary derivatives thereof. The novel compounds are suitable for the treatment of a state connected with oxygen deficit and/or energy deficit, or a disease based on PARP inhibition, especially an autoimmune or neurodegenerative disease, and/or a viral disease, and/or a disease caused by a toxic effect.
    Type: Grant
    Filed: March 21, 2005
    Date of Patent: December 19, 2006
    Assignee: N-Gene Research Laboratories Inc.
    Inventors: Peter Literati Nagy, Balazs Sumegi, Kalman Takacs
  • Patent number: 7125870
    Abstract: The present application describes novel isoxazoline of formula I or II: or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, R1, R2, R3, R4, Z, U, X, Y, Za, and n are defined in the present specification, which are useful as inhibitors of matrix metalloproteinases (MMP), TNF-? converting enzyme (TACE), or a combination thereof.
    Type: Grant
    Filed: October 30, 2003
    Date of Patent: October 24, 2006
    Assignee: Bristol-Myers Squibb Company
    Inventors: Chu-Biao Xue, Thomas P. Maduskuie, Stephen E. Mercer
  • Patent number: 7122547
    Abstract: The invention relates to anthranilic acid amides and the use thereof as medicaments for the treatment of diseases that are triggered by persistent angiogenesis, in addition to intermediate products in the production of anthranilic acid amides.
    Type: Grant
    Filed: November 9, 1999
    Date of Patent: October 17, 2006
    Assignees: Schering AG, Novartis AG
    Inventors: Andreas Huth, Dieter Seidelmann, Karl-Heinz Thierauch, Guido Bold, Paul William Manley, Pascal Furet, Jeanette Marjorie Wood, Jürgen Mestan, Jose Brüggen, Stefano Ferrari, Martin Krüger, Eckhard Ottow, Andreas Menrad, Michael Schirner
  • Patent number: 7094899
    Abstract: This invention relates to a vitreous form of 8-[3-[N-[(E)-3-(6-acetamidopyridin-3-yl)acryloylglycyl]-N-methylamino]-2,6-dichlorobenzyloxy]-2-methylquinoline (FR173657). This vitreous form has good solid stability and, therefor, is useful for producing and supplying FR173657 products whose quality is stable enough to be suitable for medicines.
    Type: Grant
    Filed: November 22, 2002
    Date of Patent: August 22, 2006
    Assignee: Astellas Pharma Inc.
    Inventors: Norio Ohnishi, Osamu Aoki, Atsuo Ohike, Kazuto Okimoto, Hiroshi Ishikuro
  • Patent number: 7071192
    Abstract: The present invention concerns compounds of formula (I), prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms thereof wherein -a1=a2-a3=a4-represents a radical of formula —CH?CH—CH?CH—; —N—CH—CH?CH—; —CH?N—CH?CH—; —CH?CH—N?CH—; —CH?CH—CH?N—; wherein each hydrogen atom may optionally be substituted; Q is a radical of formulae (b-1), (b-2), (b-3), (b-4), (b-5), (b-6), (b-7) and (b-8), wherein Alk is C1-6alkanediyl; Y1 is a bivalent radical of formula —NR2— or —CH(NR2R4)—; X1 is NR4, S, S(?O), S(?O)2, O, CH2, C(?O), CH(?CH2), CH(OH), CH(CH3), CH(OCH3), CH(SCH3), CH(NR5aR5b), CH2—NR4 or NR4—CH2; X2 is a direct bond, CH2, C(?O), NR4, C1-4alkyl-NR4, NR4—C1-4alkyl, t is 2 to 5; u is 1 to 5; v is 2 or 3; and whereby each hydrogen in Alk and in (b-3), (b-4), (b-5), (b-6), (b-7) and (b-8), may optionally be replaced by R3: provided that when R3 is hydroxy or C1-6alkyloxy, then R3 cannot replace a hydrogen atom in the a position relative to a nitrogen atom; G is a di
    Type: Grant
    Filed: June 20, 2000
    Date of Patent: July 4, 2006
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Frans Eduard Janssens, Jean Fernand Armand Lacrampe, Jérôme Emile Georges Guillemont, Marc Gaston Venet, Koenraad Jozef Lodewijk Marcel Andries
  • Patent number: 7041667
    Abstract: Compounds of Formula 1 [Region ?]—[Region ?]—[Region ?]—[Region ?]??(1) which are useful as modulators of chemokine activity. The invention also provides pharmaceutical formulations and methods of treatment using these compounds.
    Type: Grant
    Filed: December 1, 1999
    Date of Patent: May 9, 2006
    Assignee: Pfizer, Inc.
    Inventors: Duncan Robert Armour, David Anthony Price, Blanda Luzia Christa Stammen, Anthony Wood, Manoussos Perros, Martin Paul Edwards
  • Patent number: 6995162
    Abstract: Selected heterocyclic compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
    Type: Grant
    Filed: January 10, 2002
    Date of Patent: February 7, 2006
    Assignee: Amgen Inc.
    Inventors: Guoqing Chen, Jeffrey Adams, Jean Bemis, Shon Booker, Guolin Cai, Lucian Di Pietro, Celia Dominguez, Daniel Elbaum, Julie Germain, Stephanie Geuns-Meyer, Michael Handley, Qi Huang, Joseph L. Kim, Tae-Seong Kim, Alexander Kiselyov, Xiaohu Ouyang, Vinod F. Patel, Leon M. Smith, Markian Stec, Andrew Tasker, Ning Xi, Shimin Xu, Chester Chenguang Yuan, Michael Croghan
  • Patent number: 6962942
    Abstract: The present invention is directed to non-peptidic factor Xa inhibitors which are useful for the treatment of arterial and venous thrombotic occlusive disorders, inflammation, cancer, and neurodegenerative diseases. The factor Xa inhibitors provide compounds having Formula I: or pharmaceutically acceptable salts thereof; wherein Q is phenyl, benzyl, pyridyl, thienyl, indolyl, quinolinyl, benzothienyl, biphenylyl, or imidazolyl; any of which can include one or more optional substituents independently selected from halo, trifluoromethyl, hydroxy, amino, nitro, cyano, C1 alkoxy, C1-3 alkyl, methylenedioxy, carboxamido, acetamido, or amidino; X is methylene, carbonyl, or sulfonyl; Z is methylene, ethylene, or propylene; M is methylene or ethylene; and R1 R2 and R3 are independently hydrogen or C1-3 alkyl.
    Type: Grant
    Filed: September 16, 2002
    Date of Patent: November 8, 2005
    Assignee: 3-Dimensional Pharmaceuticals, Inc.
    Inventors: Scott C. Miller, Juan José Marugán Sánchez, Kristin D. Haslow, Jonathan Hall
  • Patent number: 6958349
    Abstract: This invention is directed towards novel alkylamide derivatives as bradykinin receptor antagonists useful for the treatment of bradykinin modulated disorders such as pain, inflammation, asthma and allergy. Furthermore, the present invention is directed to novel alkylamide derivatives as bradykinin receptor agonists useful for the treatment of bradykinin modulated disorders such as hypertension and the like.
    Type: Grant
    Filed: March 31, 2003
    Date of Patent: October 25, 2005
    Assignee: Ortho-McNeil Pharmaceuticals, Inc.
    Inventors: John R. Carson, Michele C. Jetter, Jung S. Lee, Mark A. Youngman
  • Patent number: 6903094
    Abstract: The present invention relates to a compound of the formula [1?] ? wherein R2 is lower alkyl optionally substituted by hydroxy, amino and the like, ring B is phenyl, thienyl and the like, E is a single bond, —O—, —S— and the like, ring G is aryl, heterocyclic group and the like, R5 is halogen atom, hydroxy, lower alkyl optionally substituted by halogen atom etc., and the like, t is 0 or an integer of 1 to 5, when t is an integer of 2 to 5, each R5 may be the same or different, m is 0 or an integer of 1 to 8, and n is 0 or an integer of 1 to 4, and a nociceptin antagonist containing compound [1?] as an active ingredient. The compound [1?] shows, due to nociceptin antagonistic action, analgesic effect against sharp pain such as postoperative pain and the like. The present invention also relates to the use of certain amide derivative inclusive of compound [1?] as a nociceptin antagonist or analgesic.
    Type: Grant
    Filed: May 10, 2002
    Date of Patent: June 7, 2005
    Assignee: Japan Tabacco, Inc.
    Inventors: Hisashi Shinkai, Takao Ito, Hideki Yamada
  • Patent number: 6900210
    Abstract: The present invention provides novel heterocyclic amides and related derivatives having the general Formula I wherein R1, R2, R3, R4, R5, R6, A, B and Z are as defined in the specification, or a nontoxic pharmaceutically acceptable salt, solvate or hydrate thereof which are openers or activators of KCNQ potassium channels. The present invention also provides pharmaceutical compositions comprising said heterocyclic amides and to the method of treatment of disorders sensitive to KCNQ potassium channel opening activity such as migraine or a migraine attack, bipolar disorders, epilepsy, acute and chronic pain and anxiety.
    Type: Grant
    Filed: November 21, 2003
    Date of Patent: May 31, 2005
    Assignee: Bristol-Myers Squibb Company
    Inventors: Yong-Jin Wu, Li-Qiang Sun, Jie Chen, Huan He
  • Patent number: 6884808
    Abstract: Described is a heterocycle-containing carboxylic acid derivative represented by the following formula (I): wherein A represents, for example, a heteroaryl group which contains at least one nitrogen atom and may have a substituent, B represents, for example, a heteroarylene group, a —CONH— group or a group represented by the formula —CR6?CR7— in which R6 and R7 represents H, a lower alkyl group or the like, D represents an arylene group, a heteroarylene group or the like, n1 stands for 0 or 1, M represents, for example, a hydroxyl group or a lower alkoxy group; or a physiologically acceptable salt thereof. As a retinoic-related compound replacing retinoic acid, it permits the provision of a preventive and/or therapeutic for various diseases.
    Type: Grant
    Filed: January 6, 2003
    Date of Patent: April 26, 2005
    Assignee: Eisai Co. Ltd.
    Inventors: Kouichi Kikuchi, Shigeki Hibi
  • Patent number: 6878714
    Abstract: Selected amines are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
    Type: Grant
    Filed: July 17, 2002
    Date of Patent: April 12, 2005
    Assignee: Amgen Inc.
    Inventors: Benny Askew, Jeffrey Adams, Shon Booker, Guoqing Chen, Lucian V. DiPietro, Daniel Elbaum, Julie Germain, Stephanie D. Geuns-Meyer, Gregory J. Habgood, Michael Handley, Qi Huang, Tae-Seong Kim, Aiwen Li, Nobuko Nishimura, Rana Nomak, Vinod F. Patel, Babak Riahi, Joseph L. Kim, Ning Xi, Kevin Yang, Chester Chenguang Yuan
  • Patent number: 6875884
    Abstract: Urea and thiourea derivatives inhibit cell function of the chemokine receptor CCR-3. These compounds offer an effective means for treating a range of diseases thought to be mediated by the CCR-3 receptor. A variety of useful urea and thiourea derivatives can be synthesized using liquid and solid phase synthesis protocols.
    Type: Grant
    Filed: July 28, 2000
    Date of Patent: April 5, 2005
    Assignee: Kirin Beer Kabushiki Kaisha
    Inventors: Janak Padia, Michael Hocker, Tsuyoshi Nishitoba, Hirohi Ohashi, Eiji Sawa
  • Patent number: 6849639
    Abstract: The invention comprises novel compounds that are effective in the prophylaxis and treatment of diseases, such as integrin receptors mediated diseases, in particular, diseases or conditions mediated by integrin receptors, such as a ?v?3, ?v?5, ?v?6, ?5?1 and the like. The invention encompasses novel compounds, pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of such diseases and disorders. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
    Type: Grant
    Filed: December 8, 2000
    Date of Patent: February 1, 2005
    Assignee: Amgen Inc.
    Inventors: Celia Dominguez, Guoqing Chen, Ning Xi, Shimin Xu, Nianhe Han, Qingyian Liu, Qi Huang, Aaron Siegmund, Michael Handley, Longbin Liu, Alexander Kiselyov
  • Patent number: 6846819
    Abstract: Compounds of the formula (I) are disclosed which are Fab I inhibitors and are useful in the treatment of bacterial infections.
    Type: Grant
    Filed: October 6, 2000
    Date of Patent: January 25, 2005
    Assignee: Affinium Pharmaceuticals, Inc.
    Inventors: William H. Miller, Kenneth A. Newlander, Mark A. Seefeld, Irene N. Uzinskas, Walter E. DeWolf, Jr., Dalia R. Jakas
  • Patent number: 6838466
    Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, TNF-? or combinations thereof.
    Type: Grant
    Filed: December 19, 2002
    Date of Patent: January 4, 2005
    Assignee: Schering Corporation
    Inventors: Zhaoning Zhu, Robert Mazzola, Zhuyan Guo, Brian J. Lavey, Lisa Sinning, Joseph Kozlowski, Brian McKittrick, Neng-Yang Shih
  • Publication number: 20040266818
    Abstract: The present invention relates to a novel class of hydroxamic acid derivatives having at least two aryl containing groups, at least one of which is a quinolinyl, isoquinolinyl or benzyl moiety, linked to the hydroxamic acid group through a methylene chain. The hydroxamic acid compounds can be used to treat cancer, for example, brain cancer. The hydroxamic acid compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention are also useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.
    Type: Application
    Filed: April 1, 2004
    Publication date: December 30, 2004
    Inventors: Ronald Breslow, Thomas A. Miller, Sandro Belvedere, Paul A. Marks, Victoria M. Richon, Richard A. Rifkind
  • Patent number: 6831080
    Abstract: There is provided novel cinnamide derivatives of Formula I: wherein R is C1-4 alkyl or trifluoromethyl; R1 is selected from the group consisting of pyridinyl, quinolinyl, thienyl, furanyl, 1,4-benzodioxanyl, 1,3-benzodioxolyl, chromanyl, indanyl, biphenylyl, phenyl and substituted phenyl in which said substituted phenyl is substituted with one or two substituents each independently selected-from the group consisting of halogen, C1-4 alkyl, C1-4 alkoxy, trifluoromethyl, trifluoromethoxy and nitro; R2 and R3 are each independently selected from the group consisting of hydrogen, C1-4 alkyl, and halogen; R4 is selected from the group consisting of di(C1-4 alkyl)amino, trifluoromethoxy and optionally substituted morpholin-4-yl, pyridinyl, pyrimidinyl, piperazinyl, and pyrazinyl with one or two substituents in which said substituent is independently selected from the group consisting of C1-4 alkyl, aminomethyl, hydroxymethyl, chloro or fluoro; R5 is hydrogen, chloro or fluoro; or R4 and R5 taken t
    Type: Grant
    Filed: May 31, 2002
    Date of Patent: December 14, 2004
    Assignee: Bristol-Myers Squibb Company
    Inventors: Yong-Jin Wu, Li-Quang Sun, Jie Chen, Huan He, Alexandre L'Heureux, Pierre Dextraze, Jean-Paul Daris, Gene G. Kinney, Steven I. Dworetzky, Piyasena Hewawasam
  • Patent number: 6825215
    Abstract: The present application describes novel 1,1-disubsituted cyclic derivatives of formula I: or pharmaceutically acceptable salt forms thereof, wherein ring B is a 3-8 membered non-aromatic ring consisting of: carbon atoms, 0-1 carbonyl groups, 0-1 double bonds, and from 0-2 ring heteroatoms selected from O, N, NR2, S, S(O), and S(O)2 and the other variables are defined in the present specification, which are useful as metalloprotease and as TNF-&agr; inhibitors.
    Type: Grant
    Filed: January 9, 2002
    Date of Patent: November 30, 2004
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Xiao-Tao Chen, Chu-Biao Xue
  • Patent number: 6809105
    Abstract: Compounds of formula I pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals.
    Type: Grant
    Filed: April 12, 2001
    Date of Patent: October 26, 2004
    Assignee: Abbott Laboratories
    Inventors: Michael R. Schrimpf, Karin R. Tietje, Richard B. Toupence, Jianguo Ji, Anwer Basha, William H. Bunnelle, Jerome F. Daanen, Jennifer M. Pace, Kevin B. Sippy
  • Patent number: 6794336
    Abstract: The present invention relates to a compound of the formula (I) or salt thereof in which R1 is identical or different at each occurrence and is H, halogen, CN, nitro, SF5, (C1-C8)alkyl, (C2-C8)alkenyl, (C2-C8)alkynyl, (C1-C8)alkoxy, [(C1-C8)alkyl]-carbonyl or (C1-C8)alkylsulfonyl, each of the radicals being unsubstituted or substituted,  or is S(O)p—R7, where p=0, 1 or 2 and R7 is (C1-C8)alkyl, (C1-C8)haloalkyl or NR8R9, where  R8 and R9 independently of one another are identical or different and are H, (C1-C8)alkyl, (C2-C8)alkenyl, (C7-C10)arylalkyl, (C7-C10)alkylaryl or (C6-C10)aryl, each of the last-mentioned five radicals being unsubstituted or substituted,  or is a group of the formula where R10 is (C1-C8)alkyl which is unsubstituted or substituted, and W=O or S, A is optionally substituted aryl or an optionally substituted heterocyclic radical, X is O or S, R2,R3,R4, and R5 are identical or different and are H, hal
    Type: Grant
    Filed: June 21, 2002
    Date of Patent: September 21, 2004
    Assignee: Aventis Crop Science GmbH
    Inventors: Klaus Haaf, Lothar Willms, Thomas Auler, Hubert Menne, Hermann Bieringer
  • Patent number: 6784184
    Abstract: This invention relates to a method of using novel 5-(arylsulfonyl)-,5-(arylsulfinyl), and 5-(arylsulfanyl)-thiazolidine-2,4-diones of Formula (I), wherein Ar, Ar′, R6, m and n are as defined in the specification as inhibitors of Ras FPTase, and may be used as an alternative to, or in conjunction with, traditional cancer therapy for treating ras-oncogene-dependent tumors, such as cancers of the pancreas, colon, bladder, and thyroid.
    Type: Grant
    Filed: August 23, 2002
    Date of Patent: August 31, 2004
    Assignee: Wyeth Holdings Corporation
    Inventors: Joseph William Epstein, Semiramis Ayral-Kaloustian, Gary Harold Birnberg, Edward James Salaski, Gloria Jean Macewan, Katherine Cheung
  • Patent number: 6777427
    Abstract: Tetrahydroquinoline compounds of general formula (I) or pharmacologically acceptable salts thereof, which have a specific and strong binding affinity for AR, exhibit AR agonism or antagonism, have therapeutic effects on AR-mediated diseases, particularly by not acting excessively on the prostate as AR agonists, but by showing potent action on skeletal muscle tissue and bone tissue; and pharmaceutical compositions comprising the compounds or the salts as active ingredients:
    Type: Grant
    Filed: March 13, 2003
    Date of Patent: August 17, 2004
    Assignee: Kaken Pharmaceutical Co., Ltd.
    Inventors: Motonori Miyakawa, Seiji Amano, Misa Kamei, Keigo Hanada, Kazuyuki Furuya, Noriko Yamamoto
  • Patent number: 6759414
    Abstract: This application relates to a compound of formula I (or a pharmaceutically acceptable salt thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.
    Type: Grant
    Filed: July 29, 2003
    Date of Patent: July 6, 2004
    Assignee: Eli Lilly and Company
    Inventors: Douglas Wade Beight, Trelia Joyce Craft, Carl Penman Denny, Jeffry Bernard Franciskovich, Theodore Goodson, Jr., Steven Edward Hall, David Kent Herron, Sajan Joseph, Valentine Joseph Klimkowski, Jeffrey Alan Kyle, John Joseph Masters, David Mendel, Guy Milet, Marta Maria Piñeiro-Nuñez, Jason Scott Sawyer, Robert Theodore Shuman, Gerald Floyd Smith, Anne Louise Tebbe, Jennifer Marie Tinsley, Leonard Crayton Weir, James Howard Wikel, Michael Robert Wiley, Ying Kwong Yee
  • Patent number: 6756385
    Abstract: The invention provides compounds of formula 1 wherein R1, R2, R3, and R4 are as defined, and their pharmaceutically acceptable salts. Compounds of formula 1 are indicated to have activity inhibiting cdk5, cdk2, and GSK-3. Pharmaceutical compositions and methods comprising compounds of formula 1 for treating and preventing diseases and conditions comprising abnormal cell growth, such as cancer, and neurodegenerative diseases and conditions and those affected by dopamine neurotransmission.
    Type: Grant
    Filed: July 31, 2001
    Date of Patent: June 29, 2004
    Assignee: Pfizer Inc.
    Inventors: Mark A. Sanner, Chris J. Helal, Christoper B. Cooper, Frank S. Menniti, Michael K. Ahlijanian, Annabella Villalobos, Lit-Fui Lau, Patricia A. Seymour
  • Publication number: 20040110951
    Abstract: The invention provides thiazolidinedione, oxadiazolidinedione, and triazolone compounds of Formula (I) which compounds are thyroid receptor ligands.
    Type: Application
    Filed: July 11, 2003
    Publication date: June 10, 2004
    Inventor: Yuan-Ching P. Chiang
  • Patent number: 6743807
    Abstract: The present application describes novel cyclic &bgr;-amino acid derivatives of formula I: or pharmaceutically acceptable salt forms thereof, wherein ring B is a 5-7 membered cyclic system containing from 0-2 heteroatoms selected from O, N, NRa, and S(O)p, and 0-1 carbonyl groups and the other variables are defined in the present specification, which are useful as metalloprotease and/or as TNF-&agr; inhibitors.
    Type: Grant
    Filed: March 16, 2001
    Date of Patent: June 1, 2004
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Jingwu Duan, Gregory Ott, Lihua Chen, Carl Decicco, Zhonghui Lu, Thomas P. Maduskuie, Jr., Chu-Biao Xue
  • Patent number: 6740649
    Abstract: The present application describes novel cyclic hydroxamic acids of formula I: or pharmaceutically acceptable salt forms thereof, wherein ring B is a 5-7 membered cyclic system containing from 0-2 heteroatoms selected from O, N, NR1, and S(O)p, and 0-1 carbonyl groups and the other variables are defined in the present specification, which are useful as inhibitors of matrix metalloproteinases (MMP), TNF-&agr; converting enzyme (TACE), aggrecanase or a combination thereof, pharmaceutical compositions containing the same, and methods of using the same.
    Type: Grant
    Filed: September 16, 2002
    Date of Patent: May 25, 2004
    Assignee: Bristol-Myers Squibb Company
    Inventors: Gregory R. Ott, Xiao-Tao Chen, Jingwu Duan, Zhonghui Lu
  • Patent number: 6706711
    Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: wherein R1, R2, T, n and Q are as described in the specification. The compounds are useful for treating diseases in mammals that are alleviated by a protein kinase inhibitor, particularly diseases, such as cancer, inflammatory disorders, restenosis, and cardiovascular disease.
    Type: Grant
    Filed: April 26, 2002
    Date of Patent: March 16, 2004
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventor: Michael R. Hale
  • Patent number: 6693117
    Abstract: Compounds of general formula (I) are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts, pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain.
    Type: Grant
    Filed: August 19, 2002
    Date of Patent: February 17, 2004
    Assignee: AstraZeneca Canada Inc.
    Inventors: Daniel Delorme, Edward Roberts, Zhongyong Wei
  • Patent number: RE40525
    Abstract: A racemate diastereoisomer and optical isomer of a compound of formula (I): wherein B is H, a C6 or C10 aryl, C7-16 aralkyl; Het or (lower alkyl)-Het, all of which may be optionally substituted with C1-6 alkyl; C1-6 alkoxy; C1-6 alkanoyl; hydroxy; hydroxyalkyl; halo; haloalkyl; nitro; cyano; cyanoalkyl; amino optionally substituted with C1-6 alkyl; amido; or (lower alkyl)amide; or B is an acyl derivative of formula R4—C(O)—; a carboxyl derivative of formula R4—O—C(O)—; an amide derivative of formula R4—N(R5)—C(O)—; a thioamide derivative of formula R4—N(R5)—C(S)—; or a sulfonyl of formula R4—SO2; R5 is H or C1-6 alkyl; and Y is H or C1-6 alkyl; R3 is C1-8 alkyl, C3-7 cycloalkyl, or C4-10 alkylcycloalkyl, all optionally substituted with hydroxy, C1-6 alkoxy, C1-6 thioalkyl, amido, (lower alkyl)amido, C6 or C10 aryl, or C7-16 aralkyl; R2 is C2—R20, NH—R20, O—R20 or S—R20, wherein R20 is a saturated or unsaturated C3-7 cycloalkyl or C4-10 (alkylcycloalkyl), all of which being optionally mono-, di- or tri-
    Type: Grant
    Filed: September 30, 2005
    Date of Patent: September 30, 2008
    Assignee: Boehringer Ingelheim (Canada) Ltd.
    Inventors: Montse Llinas-Brunet, Murray D. Bailey, Dale R. Cameron, Anne-Marie Faucher, Elise Ghiro, Nathalie Goudreau, Teddy Halmos, Marc-André Poupart, Jean Rancourt, Youla S. Tsantrizos, Dominik M. Wernic