Chalcogen Bonded Directly To Diazine Ring Carbon Patents (Class 544/298)
  • Publication number: 20100121058
    Abstract: 2-(Substituted phenyl)-6-amino-5-alkoxy, thioalkoxy and aminoalkyl-4-pyrimidinecarboxylic acid and its derivatives are potent herbicides demonstrating broad spectrum of weed control.
    Type: Application
    Filed: November 23, 2009
    Publication date: May 13, 2010
    Applicant: DOW AGROSCIENCES LLC
    Inventors: Katherine A. Guenthenspberger, Thomas L. Siddall
  • Publication number: 20100113479
    Abstract: The present invention is directed to novel processes for the preparation of tri-substituted pyridine and tri-substituted pyrimidine derivatives, useful as glucose dependent insulinotropic receptor agonist, for the treatment of metabolic-related disorders and complications thereof, such as, diabetes and obesity.
    Type: Application
    Filed: October 29, 2009
    Publication date: May 6, 2010
    Inventors: Anusuya Choudhury, Michael Reuman
  • Publication number: 20100113276
    Abstract: The use of N2-phenylamidines of formula (I) as herbicides is described. In this formula (I), R2, R3, R4, R5 and R6 are different radicals and A is a bond or various 1- or polyatomic bridging elements.
    Type: Application
    Filed: March 4, 2008
    Publication date: May 6, 2010
    Applicant: BAYER CROPSCIENCE AG
    Inventors: Birgit Kuhn, Harald Jakobi, Thomas Mueller, Joerg Tiebes, Heinz Kehne, Dirk Schmutzler, Martin Hills, Christopher Rosinger, Klaus Kunz, Mark Wilheim Drewes, Dieter Feucht, Thomas Seitz, Benoit Hartmann, Ralf Dunkel, Joerg Nico Greul, Oliver Guth, Kerstein Ilg, Darren James Mansfeld, Wahed Ahmed Moradi, Peter Dahmen, Ulrike Wachendorf-Neumann, Arnd Voerste, Dale Robert Mitchell, Jean-Pierre Andre Vors, Dale Robert Mitchell, Tom Hough
  • Publication number: 20100113480
    Abstract: The present invention is directed to novel processes for the preparation of tri-substituted pyridine and tri-substituted pyrimidine derivatives, useful as glucose dependent insulinotropic receptor agonist, for the treatment of metabolic-related disorders and complications thereof, such as, diabetes and obesity.
    Type: Application
    Filed: October 29, 2009
    Publication date: May 6, 2010
    Inventor: Michael Reuman
  • Patent number: 7683070
    Abstract: It has now been found that certain novel N-(substituted aryl)-4-(disubstituted methyl)piperidine and pyridine derivatives have provided unexpected insecticidal activity. These compounds are represented by formula (I): wherein m, n, q, r, and s are independently selected from 0 or 1; and p is 0, 1, 2, or 3; A is C or CH; and B, D, E, R, R1, R2, R3, R4, R5, R6, R7 and R8 are fully described herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula I, and optionally, an effective amount of at least one of a second compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.
    Type: Grant
    Filed: October 17, 2007
    Date of Patent: March 23, 2010
    Assignee: FMC Corporation
    Inventors: Ping Ding, Robert N. Henrie, II, Daniel H. Cohen, John W. Lyga, David S. Rosen, George Theodoridis, Qun Zhang, Walter H. Yeager, Stephen F. Donovan, Stephen Shunxiang Zhang, Inna Shulman, Seong Jae Yu, Guozhi Wang, Y. Larry Zhang, Ariamala Gopalsamy, Dennis L. Warkentin, Paul E. Rensner, Ian R. Silverman, Thomas G. Cullen
  • Publication number: 20100069634
    Abstract: Disclosed are compounds of the formula I: wherein R1, R2, V, W, X, Y and Z can be as defined herein. The compounds can be used in the treatment of disorders mediated by the cannabinoid receptors.
    Type: Application
    Filed: October 14, 2009
    Publication date: March 18, 2010
    Inventors: Bob M. Moore, II, Steven Gurley, Suni Mustafa, Patrick Allison
  • Publication number: 20100041683
    Abstract: Compounds, preferably 5-pyrimidinol and 3-pyridinol derivatives, that act as effective chain breaking antioxidants of both the lipid and water-soluble variety (analogous to the natural Vitamins E and C), many of which are more reactive toward peroxyl radicals than the most potent form of Vitamin E. These compounds may exhibit many chemopreventive effects associated with conditions in which free radical-mediated cellular damage or disruption is implicated and Vitamins E and C are shown to have protective effects. Additionally, these compounds should be excellent oxidation inhibitors as additives to fuels, lubricants, rubber, polymers, chemicals, solvents and foodstuffs.
    Type: Application
    Filed: June 16, 2009
    Publication date: February 18, 2010
    Inventors: Derek A. Pratt, Luca Valgimigli, Gino A. DiLabio
  • Patent number: 7659300
    Abstract: The present invention is directed to compounds of Formula I: I (where A1, A2, B, J, K, m, n, R4, R5a, R5b and R5c are as defined herein) useful as antagonists of CGRP receptors and 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: September 6, 2005
    Date of Patent: February 9, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ian M. Bell, Craig A. Stump
  • Patent number: 7659271
    Abstract: A compound represented by the following general formula (I), wherein R1, R2, R3, R4 and R5 represent hydrogen atom, a halo(lower alkyl) group, cyano group and the like, R6 represents an alkyl group, a cycloalkyl group and the like, R7, R8, R9 and R10 represent hydrogen atom, a halogen atom, a lower alkyl group, a halo(lower alkyl) group and the like, R11 and R12 represent hydrogen atom, a lower alkyl group, a (lower cycloalkyl) (lower alkyl) group and the like, and R13 represents hydrogen atom, a halogen atom, a lower alkoxy group and the like, which has potent inhibitory activity on cholesterol ester transfer protein (CETP).
    Type: Grant
    Filed: April 10, 2008
    Date of Patent: February 9, 2010
    Assignee: Kowa Company, Ltd.
    Inventors: Tadaaki Ohgiya, Toru Miura, Ayumu Okuda, Toshiharu Arai, Koichi Yamazaki, Taro Aoki, Katsutoshi Miyosawa, Haruki Shibata, Kimiyuki Shibuya
  • Publication number: 20100029643
    Abstract: The invention relates to chemical compounds of formula (I), (Ia) and (Ib) or pharmaceutically acceptable salts thereof, which possess Edg-1 antagonistic activity and are accordingly useful for their anti-cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments for use in the production of an anti-cancer effect in a warm-blooded animal, such as man.
    Type: Application
    Filed: November 8, 2007
    Publication date: February 4, 2010
    Applicant: ASTRAZENECA AB
    Inventors: Gurmit Grewal, Edward Hennessy, Victor Kamhi, Danyang Li, Paul Lyne, Vibha Oza, Jamal Carlos Saeh, Qibin Su, Bin Yang
  • Patent number: 7652010
    Abstract: Azabicyclo pyridazinyl compounds including azabicyclooctyl-pyridazinyl-oxy compounds, which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile, the compounds may be used for the treatment of various diseases or disorders, including those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
    Type: Grant
    Filed: October 14, 2005
    Date of Patent: January 26, 2010
    Assignee: Neurosearch A/S
    Inventors: Dan Peters, Daniel B. Timmermann, Gunnar M. Olsen, Elsebet Østergaard Nielsen, Tino Dyhring Jørgensen
  • Patent number: 7652009
    Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF 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: November 29, 2005
    Date of Patent: January 26, 2010
    Assignee: Amgem Inc.
    Inventors: Tae-Seong Kim, Steven Bellon, Shon Booker, Noel D'Angelo, Celia Dominguez, Ingrid Fellows, Matthew Lee, Longbin Liu, Elizabeth Rainbeau, Aaron C. Siegmund, Andrew Tasker, Ning Xi, Yuan Cheng
  • Patent number: 7652041
    Abstract: The present invention provides novel cinnamide compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.
    Type: Grant
    Filed: January 12, 2006
    Date of Patent: January 26, 2010
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Ruth S. Adams, Emily F. Calderwood, Alexandra E. Gould, Paul D. Greenspan, Matthew J LaMarche, Yuan Tian, Tricia J. Vos
  • Patent number: 7642220
    Abstract: 2-(Substituted phenyl)-6-amino-5-alkoxy, thioalkoxy and aminoalkyl-4-pyrimidinecarboxylic acid and its derivatives are potent herbicides demonstrating broad spectrum of weed control.
    Type: Grant
    Filed: August 29, 2008
    Date of Patent: January 5, 2010
    Assignee: Dow AgroSciences LLC
    Inventors: Jeffrey B. Epp, Paul R. Schmitzer, Katherine A. Guenthenspberger, William C. Lo, Thomas L. Siddall
  • Patent number: 7642303
    Abstract: Thermoplastic composition and articles containing UV absorbers that protect the articles contents from harmful UV radiation are disclosed as well as methods for making the thermoplastic articles and methods for using the articles to contain and protect materials sensitive to UV radiation. The UV absorbers contain oxazolone and/or azine functional groups that absorb UV radiation and prevent its transmission into the article. Many of the compounds are novel compositions of matter. The generally clear thermoplastic articles of this disclosure are particularly useful for containing a variety of UV sensitive consumer products that would otherwise have to be packaged in opaque containers.
    Type: Grant
    Filed: October 13, 2005
    Date of Patent: January 5, 2010
    Inventors: Thomas L. Shakely, James John Krutak
  • Publication number: 20090291971
    Abstract: The present invention relates to processes for the preparation of heteroaryl ethers. In some embodiments, the processes relate to cross coupling reactions between triazol-1-yloxy and triazol-1-yl heterocycles with aryl boronic acids. In a further aspect, this invention also relates to compounds that are useful for the treatment of oncological diseases or disorders, and for the treatment of inflammation.
    Type: Application
    Filed: October 30, 2008
    Publication date: November 26, 2009
    Applicant: Wyeth
    Inventors: Tarek Suhayl Mansour, Sumrit Wacharasindhu, Zhao-Kui Wan, Sujata Bardhan
  • Publication number: 20090275591
    Abstract: The present invention provides a compound having a superior acid secretion inhibitory effect and showing an antiulcer activity and the like. The present invention provides a compound represented by the formula (I) wherein R1 is a nitrogen-containing monocyclic heterocyclic group optionally condensed with a benzene ring or a heterocycle, the nitrogen-containing monocyclic heterocyclic group optionally condensed with a benzene ring or a heterocycle optionally has substituent(s), R2 is an optionally substituted C6-14 aryl group, an optionally substituted thienyl group or an optionally substituted pyridyl group, R3 and R4 are each a hydrogen atom, or one of R3 and R4 is a hydrogen atom and the other is an optionally substituted lower alkyl group, an acyl group, a halogen atom, a cyano group or a nitro group, and R5 is an alkyl group or a salt thereof.
    Type: Application
    Filed: August 29, 2006
    Publication date: November 5, 2009
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMTED
    Inventors: Masahiro Kajino, Atsushi Hasuoka, Haruyuki Nishida
  • Patent number: 7598423
    Abstract: This application relates to a substituted hydroxyphenyl ketone compound of formula I, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition thereof and its use in treating migraine. This application also relates to processes for preparing a compound of formula I, and intermediate compounds useful therein.
    Type: Grant
    Filed: November 15, 2005
    Date of Patent: October 6, 2009
    Assignee: Eli Lilly and Company
    Inventors: Thomas Daniel Aicher, Guillermo S. Cortez, Todd Michael Groendyke, Albert Khilevich, James Allen Knobelsdorf, Fredrik Pehr Marmsater, Jeffrey Michael Schkeryantz, Tony Pisal Tang, Nicholas Andrew Magnus
  • Publication number: 20090240053
    Abstract: The invention is directed to substituted 2-aminoacetamides represented by formula (II): and to pharmaceutically acceptable salts and prodrugs thereof, wherein the substituents are defined herein. The invention is also directed to the use of substituted 2-aminoacetamides in methods for the treatment of neuronal damage following global and focal ischemia, and for the treatment, prevention or amelioration of pain, as anticonvulsants, as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.
    Type: Application
    Filed: May 28, 2009
    Publication date: September 24, 2009
    Applicant: Purdue Neuroscience Company
    Inventors: Nancy C. Lan, Yan Wang, Sui Xiong Cai
  • Patent number: 7589090
    Abstract: Compounds and methods for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist, the compounds being of formula (I): wherein R1, R2, R3 and R4 are as defined herein.
    Type: Grant
    Filed: February 27, 2008
    Date of Patent: September 15, 2009
    Assignee: Roche Palo Alto LLC
    Inventors: Michael Patrick Dillon, Alam Jahangir
  • Patent number: 7566683
    Abstract: Ethylene derivatives of formula (I): where Q is an unsubstituted or substituted phenyl or heterocyclic group, especially a 4-thiazolyl, 1- or 3-pyrazolyl, 1,3-oxazol-4-yl, phenyl or pyridyl group; E is a substituent such as a cyano group; A is a substituent such as a 4-pyrazolyl or thiazolyl group; and B is a substituent such as an alkylcarbonyl group. Agricultural chemicals and agents for preventing the attachment of aquatic organisms containing one or more such ethylene derivatives.
    Type: Grant
    Filed: August 15, 2005
    Date of Patent: July 28, 2009
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Tomoyuki Ogura, Hiroshi Murakami, Akira Numata, Rika Miyachi, Toshiro Miyake, Norihiko Mimori, Shinji Takii
  • Patent number: 7547700
    Abstract: The invention relates to compounds of general formula (1) in which X and Y=a carbon with a bonded hydrogen atom (CH) or a nitrogen atom, A=a methyl, fluoromethyl, cyano, hydroxyl, methoxy group, or a chlorine or fluorine atom on condition that when A=methyl (CH3) and X and Y both=a carbon bonded to a hydrogen atom, then B=a chlorine atom, B=a chlorine or a fluorine atom, D=a hydrogen, chlorine, fluorine atom, or a cyano or trifluoromethyl group and E=a hydrogen, fluorine or chlorine atom.
    Type: Grant
    Filed: June 18, 2003
    Date of Patent: June 16, 2009
    Assignee: PIERRE Fabre Medicament
    Inventors: Bernard Vacher, Bernard Bonnaud, Jean-Louis Maurel, Francis Colpaert
  • Patent number: 7547782
    Abstract: The present invention is directed to compounds having the formula I or II: including salts thereof, and methods for using them for the treatment of cancer.
    Type: Grant
    Filed: September 28, 2006
    Date of Patent: June 16, 2009
    Assignee: Bristol-Myers Squibb Company
    Inventors: Robert M. Borzilleri, Xiao-Tao Chen, David K. Williams, John S. Tokarski, Robert F. Kaltenbach
  • Patent number: 7547704
    Abstract: 2? and/or 3? prodrugs of 1?, 2?, 3? or 4?-branched nucleosides, and their pharmaceutically acceptable salts and derivatives are described. These prodrugs are useful in the prevention and treatment of Flaviviridae infections, including HCV infection, and other related conditions. Compounds and compositions of the prodrugs of the present invention are described. Methods and uses are also provided that include the administration of an effective amount of the prodrugs of the present invention, or their pharmaceutically acceptable salts or derivatives. These drugs may optionally be administered in combination or alteration with further anti-viral agents to prevent or treat Flaviviridae infections and other related conditions.
    Type: Grant
    Filed: December 6, 2004
    Date of Patent: June 16, 2009
    Assignees: Idenix Pharmaceuticals, Inc., Centre National de la Recherche Scientifique, Universita Degli Studi di Cagliari
    Inventors: Paola LaColla, Richard Storer, Gilles Gosselin, Jean-Pierre Sommadossi
  • Patent number: 7538072
    Abstract: A stem/leaf desiccant for crop plants which comprises as an active ingredient, a compound of formula (I): wherein X represent CH or nitrogen; Z represents halogen; A represents oxygen, sulfur, or NH; R1 represents hydroxyl, C1-C7 alkoxy, C3-C7 alkenyloxy, C3-C7 alkynyloxy, C5-C7 cycloalkoxy, {(C1-C7 alkoxy)carbonyl} C1-C3 alkoxy, (C1-C7 alkylamino)oxy, {di(C1-C7 alkyl)amino}oxy, (C3-C7 alkylideneamino)oxy, C1-C7 alkylamino, di(C1-C7 alkyl)amino, C3-C7 alkenylamino, C3-C7 alkynylamino, C5-C7 cycloalkylamino, {(C1-C7 alkoxy)carbonyl} C1-C3 alkylamino, or (C1-C7 alkoxy)amino; R2 is hydrogen or methyl; and R3 is hydrogen, halogen, C1-C3 alkyl, or C1-C3 alkoxy; a method for desiccating a crop plant and a method for harvesting a crop by using the stem/leaf desiccant.
    Type: Grant
    Filed: June 16, 2006
    Date of Patent: May 26, 2009
    Assignee: Sumitomo Chemical Company, Limited
    Inventor: Nobuaki Mito
  • Patent number: 7531547
    Abstract: Compounds and methods for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist, the methods comprising administering to a subject in need thereof an effective amount of a compound of formula (I): wherein D, X, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein.
    Type: Grant
    Filed: August 25, 2006
    Date of Patent: May 12, 2009
    Assignee: Roche Palo Alto LLC
    Inventors: Michael Patrick Dillon, Alam Jahangir, Amy Geraldine Moore, Paul J. Wagner
  • Publication number: 20090105269
    Abstract: Compositions comprising multifunctional agents and methods of use thereof are provided.
    Type: Application
    Filed: September 25, 2008
    Publication date: April 23, 2009
    Inventors: Peter F. Kador, Hongxia Jin
  • Publication number: 20090093491
    Abstract: Objects of the present invention are the compounds of formula I their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, pharmaceutical compositions containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.
    Type: Application
    Filed: September 28, 2006
    Publication date: April 9, 2009
    Inventors: Wolfgang Jenni, Thomas Von Hirschheydt, Edgar Voss
  • Publication number: 20090062125
    Abstract: 2-(Substituted phenyl)-6-amino-5-alkoxy, thioalkoxy and aminoalkyl-4-pyrimidinecarboxylic acid and its derivatives are potent herbicides demonstrating broad spectrum of weed control.
    Type: Application
    Filed: August 29, 2008
    Publication date: March 5, 2009
    Inventors: Jeffrey B. Epp, Paul R. Schmitzer, Katherine A. Guenthenspberger, William C. Lo, Thomas L. Siddall
  • Publication number: 20090062306
    Abstract: A compound represented by the following general formula (I), wherein R1, R2, R3, R4 and R5 represent hydrogen atom, a halogen atom, a lower alkyl group and the like, R6 represents an alkyl group, a cycloalkyl group and the like, R7 and R8 represent hydrogen atom, a lower alkyl group, a (lower cycloalkyl)(lower alkyl) group and the like, R9 represents hydrogen atom, a halogen atom, a lower alkoxy group and the like, R10 and R11 represent hydrogen atom, a lower alkyl group, a lower alkoxy group, a halo(lower alkyl) group and the like, and A represents a heterocyclic ring constituted by 6 to 10 atoms, which has potent inhibitory activity on cholesterol ester transfer protein (CETP).
    Type: Application
    Filed: March 11, 2008
    Publication date: March 5, 2009
    Applicant: KOWA COMPANY, LTD.
    Inventors: Tadaaki OHGIYA, Toru MIURA, Ayumu OKUDA, Toshiharu ARAI, Koichi YAMAZAKI, Taro AOKI, Katsutoshi MIYOSAWA, Haruki SHIBATA, Kimiyuki SHIBUYA
  • Patent number: 7491728
    Abstract: The pyrimidinone compounds are disclosed. Methods of preparing the pyrimidinone compounds are also disclosed.
    Type: Grant
    Filed: April 7, 2004
    Date of Patent: February 17, 2009
    Assignee: SmithKline Beecham Corp.
    Inventors: Irina V. Shcherbakova, Manuel F. Balanddrin, Guangfei Huang, Otto Geoffroy, John Fox, Robert Marquis, Dennis Shinji Yamashita, Juan Luengo, Wenyong Wang
  • Patent number: 7491827
    Abstract: The present invention provides compounds of general formula I: or a pharmaceutically acceptable salt thereof, wherein R1, X, Z, R2, X1, Ar, n, R3 and R4 are defined generally and in subsets herein. Compounds of the invention are inhibitors of CCR8 and accordingly are useful for the treatment of a variety of inflammatory and allergic disorders.
    Type: Grant
    Filed: July 14, 2004
    Date of Patent: February 17, 2009
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Mingshi Dai, Bing Guan, Robert A. Bennett, Douglas F. Burdi, Shomir Ghosh, Gang Li, Charles Minor, Tracy J. Jenkins
  • Publication number: 20090042910
    Abstract: The invention concerns quinoline derivatives of Formula I or a pharmaceutically-acceptable salt thereof, wherein each of X1, p, R1, q, R2, R3, R4, R5, Ring A, r and R6 has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders.
    Type: Application
    Filed: March 1, 2007
    Publication date: February 12, 2009
    Inventors: Frederic Henri Jung, Patrick Ple
  • 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: 20090023729
    Abstract: The present invention relates to a compound of the general formula (1): wherein, Y is a methylene group, and the like; A is an optionally substituted heterocyclic group, and the like; B is an optionally substituted heterocyclic group, and the like; R1 is an optionally substituted alkyl group, wherein the alkyl group further may optionally be substituted by an optionally substituted homocyclic group, and the like; and R2 is an optionally substituted amino group, and the like; or a pharmaceutically acceptable derivative thereof, which has an inhibitory activity against cholesteryl ester transfer protein (CETP), thereby being useful for prophylaxis and/or treatment of arteriosclerotic diseases, hyperlipemia or dyslipidemia, and the like.
    Type: Application
    Filed: July 28, 2008
    Publication date: January 22, 2009
    Applicant: Mitsubishi Tanabe Pharma Corporation
    Inventors: Yoshinori Nakamura, Norimitsu Hayashi, Takanori Higashijima, Hitoshi Kubota, Kozo Oka
  • Publication number: 20090005404
    Abstract: The present invention relates to the use of a compound of formula (I) wherein R1 is pyridyl or thiazolyl, any of which may optionally be substituted with C1-8alkyl or C2-8alkenyl; and a) R2 is methoxy and n is zero or one; or b) R2 is chlorine and n is zero and pharmaceutically acceptable salts thereof for lowering or controlling proteinuria, in particular for the treatment of diabetic nephropathy.
    Type: Application
    Filed: July 28, 2008
    Publication date: January 1, 2009
    Inventor: Jessica Mann
  • 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
  • Publication number: 20080269252
    Abstract: The invention relates to the use of compounds derived from pyrimidinetrione of general formula (I) as acetyl cholinesterase (AChE) inhibitors. The invention also relates to the use of said compounds as insecticides, and to compositions containing the same.
    Type: Application
    Filed: February 10, 2006
    Publication date: October 30, 2008
    Applicants: CENTRAL NATIONAL DE LA RECHERCHE SCIENTIFIQUE, UNIVERSITE DE MONTPELLIER 2
    Inventors: Mylene Weill, Philippe Fort, Jean-Paul Leonetti
  • Publication number: 20080269267
    Abstract: Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant melanomas, solid tumors, glioblastomas, ovarian cancer, pancreatic cancer, prostate cancer, lung cancers, breast cancers, kidney cancers, hepatic cancers, cervical carcinomas, metastasis of primary tumor sites, myeloproliferative diseases, chronic myelogenous leukemia, leukemias, papillary thyroid carcinoma, non-small cell lung cancer, mesothelioma, hypereosinophilic syndrome, gastrointestinal stromal tumors, colonic cancers, ocular diseases characterized by hyperproliferation leading to blindness including various retinopathies, diabetic retinopathy, rheumatoid arthritis, asthma, chronic obstructive pulmonary disease, mastocytosis, mast cell leukemia, a disease caused by c-Abl kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof, a disease caused by c-Kit kinase, oncogenic forms thereof, aberrant fusion proteins thereof a
    Type: Application
    Filed: April 18, 2008
    Publication date: October 30, 2008
    Applicant: Deciphera Pharmaceuticals, LLC
    Inventors: Daniel L. Flynn, Peter A. Petillo, Michael D. Kaufman
  • Patent number: 7442701
    Abstract: The present invention provides a compound of formula (I): wherein V represents NR5, O, S, SO or S(O)2; W and X each independently represent CH or N; Y represents N, CH or C—Ar2, with the proviso that at least one, but no more than two, of W, X and Y are N; Z represents CH or C—Ar2, with the proviso that when Y is N or CH then Z is C—Ar2, and with the further proviso that when Y is C—Ar2 then Z is CH; Ar1 represents a fused 9 or 10 membered heterobicyclic ring system containing one, two, three or four heteroatoms selected from nitrogen, oxygen and sulfur, wherein at least one of the rings in said ring system is aromatic; Ar2 represents an aromatic ring selected from phenyl, pyridyl, pyrimidinyl and pyridazinyl which is optionally fused and substituted; R1 represents halogen, hydroxy, oxo, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, haloC1-6alkyl, hydroxyC1-6alkyl, C1-6alkoxy, haloC1-6alkoxy, hydroxyC1-6alkoxy, C3-7cycloalkyl, C3-7cycloalkoxy, C3-5cycloalkylC1-4alkyl, cyano, nitro, SR6, SOR6, SO2R6, COR6, NR3COR6, CON
    Type: Grant
    Filed: November 14, 2003
    Date of Patent: October 28, 2008
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Peter Blurton, Frank Burkamp, Stephen Robert Fletcher, Gregory John Hollingworth, A. Brian Jones, Edward Giles McIver, Christopher Richard Moyes, Lauren Rogers
  • Publication number: 20080255166
    Abstract: The invention relates to the use of dithiocarbamate derivatives for the therapeutic or prophylactic treatment of infectious diseases in mammals (humans and animals) caused by bacteria, especially diseases like tuberculosis (TB) and lepra caused by mycobacteria and infectious diseases caused by staphylococci. The invention further relates to novel dithiocarbamate derivatives of the formula (I), wherein X is a bivalent residue selected from the group consisting of formulae having excellent antibacterial activities, and to pharmaceutical preparations containing the same.
    Type: Application
    Filed: June 6, 2008
    Publication date: October 16, 2008
    Applicant: NEED PHARMACEUTICALS S.r.I.
    Inventors: Ute Mollmann, Vadim Makarov
  • Patent number: 7429667
    Abstract: The invention concerns compounds which inhibit MEK and which have activity as anti-neoplastic agents. These compounds include N-substituted-3-hydroxy-5-arylamino-isothiazole-4-carboxamidines. Also included are the tautomeric isothiazol-3(2H)-ones.
    Type: Grant
    Filed: January 20, 2006
    Date of Patent: September 30, 2008
    Assignee: Ardea Biosciences, Inc.
    Inventors: Hassan Abdellaoui, Robert Tam, Huanming Chen, Varaprasad Chamakura, Dinesh Barawkar, Andreas Maderna, Zhi Hong, Stanley Lang
  • Publication number: 20080221078
    Abstract: The present invention discloses and claims a method of treating cognition deficits in a patient suffering from schizophrenia by administering to said patient a therapeutically effective amount of a CB1 receptor antagonist as described herein. In another aspect, this invention also discloses and claims a combination of one or more CB1 receptor antagonists and of one or more antipsychotic agents useful in the treatment of psychiatric disorders. The combination of this invention provides synergistic results in that the combination improves positive and negative symptoms of schizophrenia, weight gain and catalepsy.
    Type: Application
    Filed: May 22, 2008
    Publication date: September 11, 2008
    Applicant: AVENTIS PHARMACEUTICALS INC.
    Inventors: Mark BLACK, Beth BOROWSKY, Nancy ROGACKI, Yaw SENYAH, Rachel STEVENS
  • Publication number: 20080221139
    Abstract: The invention provides compounds of formula (I): wherein R1 and R2 are as defined in the specification; processes for their preparation; pharmaceutical compositions containing them; a process for preparing the pharmaceutical compositions; and their use in therapy. The compounds are useful as MMP inhibitors.
    Type: Application
    Filed: November 28, 2007
    Publication date: September 11, 2008
    Inventors: David Chapman, Balint Gabos, Magnus Munck af Rosenschold
  • Publication number: 20080207619
    Abstract: Compounds and methods for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist, the compounds being of formula (I): wherein R1, R2, R3 and R4 are as defined herein.
    Type: Application
    Filed: February 27, 2008
    Publication date: August 28, 2008
    Inventors: Michael Patrick Dillon, Alam Jahangir
  • Publication number: 20080207655
    Abstract: Compounds of formula (I): wherein R1 and R2 are as defined herein. Also disclosed are methods of making and using the subject compounds.
    Type: Application
    Filed: February 27, 2008
    Publication date: August 28, 2008
    Inventors: Michael Patrick Dillon, Daisy Joe Du Bois, Alam Jahangir
  • Publication number: 20080188468
    Abstract: The invention relates to substituted para-trifluoromethyl phenyl ether compounds and its preparation and use thereof especially. The substituted para-trifluoromethyl phenyl ether compounds of the invention having general formula (I): The substitutes see Description. The compounds of present invention have broad-spectrum activity, and may be used to control diseases in all sorts of plants caused by oomycete, basidiomycete, ascomycete pathogens and deuteromycete, and it may also provide good control efficacy at very low dosage because of the high activity. The compounds of the invention have good insecticidal activity and have good activity against many pests, especially for Carmine spider mite. The compounds are fit for synthetical control against many kinds of pests.
    Type: Application
    Filed: June 15, 2006
    Publication date: August 7, 2008
    Applicants: SHENYANG RESEARCH INSTITUTE OF CHEMICAL INDUSTRY, SINOCHEM CORPORATION
    Inventors: Changling Liu, Huiwei Chi, Dongliang Cui, Miao Li, Zhinian Li, Yanmei Luo, Jing Yuan
  • Patent number: 7390815
    Abstract: This invention describes novel pyrazole compounds of formula II: wherein Ring C is selected from a phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, or 1,2,4-triazinyl ring, and R2, R2?, Rx, and Ry are as described in the specification. Ring C has an ortho substituent and is optionally substituted in the non-ortho positions. R2 and R2? are optionally taken together with their intervening atoms to form a fused ring system, such as an indazole ring; and Rx and Ry are optionally taken together with their intervening atoms to form a fused ring system, such as a quinazoline ring. The compounds are useful as protein kinase inhibitors, especially as inhibitors of GSK-3, for treating diseases such as diabetes and Alzheimer's disease.
    Type: Grant
    Filed: October 23, 2003
    Date of Patent: June 24, 2008
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Robert Davies, David Bebbington, Ronald Knegtel, Marion Wannamaker, Pan Li, Cornelia Forster, Albert Pierce
  • Publication number: 20080146569
    Abstract: The present invention relates to compounds of formula (I) and pharmaceutically acceptable salts and solvates thereof, wherein the substituents are as defined herein, compositions containing such compounds and the uses of such compounds for the treatment of various diseases and conditions such as asthma.
    Type: Application
    Filed: December 12, 2007
    Publication date: June 19, 2008
    Inventors: Tanisha D. Blake, Bruce C. Hamper, Wei Huang, James R. Kiefer, Joseph B. Moon, Bradley E. Neal, Kirk L. Olson, Matthew J. Pelc, Barbara A. Schweitzer, Atli Thorarensen, John I. Trujillo, Steven R. Turner
  • Publication number: 20080146596
    Abstract: Multicyclic compounds, pharmaceutical compositions comprising them, and methods of their use are described.
    Type: Application
    Filed: November 5, 2007
    Publication date: June 19, 2008
    Inventors: Joseph Barbosa, Yingzhi Bi, Cynthia Anne Fink, Michael Alan Green, Jian Cheng Wang