Ring Sulfur In The Bicyclo Ring System Patents (Class 514/301)
  • DIAZABICYCLIC CENTRAL NERVOUS SYSTEM ACTIVE AGENTS
    Publication number: 20120208820
    Abstract: Compounds of formula I pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals.
    Type: Application
    Filed: January 31, 2012
    Publication date: August 16, 2012
    Inventors: Michael R. Schrimpf, Karin R. Tietje, Richard B. Toupence, Jianguo Ji, Anwer Basha, William H. Bunnelle, Jerome F. Daanen, Jennifer M. Frost, Kevin B. Sippy
  • AZABENZOTHIAZOLE COMPOUNDS, COMPOSITIONS AND METHODS OF USE
    Publication number: 20120202788
    Abstract: Provided are compounds of Formula I, stereoisomers, tautomers, solvates, prodrugs and pharmaceutically acceptable salts thereof, wherein A, X, R1, R2, R4 and R5 are defined herein, a pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, methods of using the compound or composition in therapy, and methods of manufacturing a compound of Formula I.
    Type: Application
    Filed: September 14, 2011
    Publication date: August 9, 2012
    Inventors: Toby Jonathan Blench, Charles Ellwood, Simon Charles Goodacre, Yingjie Lai, Jun Liang, Calum Macleod, Steven R. Magnuson, Vickie H. Tsui, Karen Williams, Birong Zhang
  • Crystal Forms of Kinase Inhibitors
    Publication number: 20120202844
    Abstract: Citrate salts of N-(4-{4-amino-7-[1-(2-hydroxyethyl)-1H-pyrazol-4-yl]thieno[3,2-c]pyridin-3-yl}phenyl)-N?-(3-fluorophenyl)urea and crystalline forms thereof are suitable pharmaceutical ingredients for pharmaceutical compositions useful in the treatment of disease, for example, cancer.
    Type: Application
    Filed: June 8, 2011
    Publication date: August 9, 2012
    Applicant: ABBOTT LABORATORIES
    Inventors: Geoff G. Z. Zhang, Doug H. Hoffman, Jonathan Miller
  • 2-HETEROARYLCARBOXYLIC ACID AMIDES
    Publication number: 20120202842
    Abstract: The invention relates to novel 2-heteroarylcarboxamides, processes for their preparation, and their use for producing medicaments for the treatment and/or prophylaxis of diseases and for improving perception, concentration, learning and/or memory.
    Type: Application
    Filed: November 4, 2011
    Publication date: August 9, 2012
    Applicant: Bayer Schering Pharma AG
    Inventors: Martin Hendrix, Frank-Gerhard Böß, Christina Erb, Timo Fleßner, Marja van Kampen, Joachim Luithle, Christoph Methfessel, Welf-Burkhard Wiese
  • LACTAM-CONTAINING COMPOUNDS AND DERIVATIVES THEREOF AS FACTOR XA INHIBITORS
    Publication number: 20120201816
    Abstract: The present application describes lactam-containing compounds and derivatives thereof of Formula I: P4—P-M-M4??I or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5-7 membered carbocycle or heterocycle and ring M is a 5-7 membered carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.
    Type: Application
    Filed: April 12, 2012
    Publication date: August 9, 2012
    Applicant: BRISTOL-MYERS SQUIBB COMPANY
    Inventors: Donald J. P. Pinto, Mimi L. Quan, Michael J. Orwat, Yun-Long Li, Wei Han, Jennifer X. Qiao, Patrick Y. S. Lam, Stephanie L. Koch
  • Pharmaceutical compositions comprising prasugrel and cyclodextrin derivatives and methods of making and using the same
    Patent number: 8236782
    Abstract: The present invention is directed to pharmaceutical compositions comprising prasugrel and a cyclodextrin derivative, and methods of making and using the same.
    Type: Grant
    Filed: May 13, 2010
    Date of Patent: August 7, 2012
    Assignee: Cydex Pharmaceuticals, Inc.
    Inventors: Gerold L. Mosher, Stephen G. Machatha, Daniel J. Cushing
  • HETEROCYCLIC COMPOUND AND ITS USE FOR CONTROL OF AN ARTHROPOD PEST
    Publication number: 20120196891
    Abstract: A heterocyclic compound represented by formula (1): wherein A1, A2, R1, R2, R3, R4, n and so on are defined in tha description, has an excellent control effect on arthropod pests and is useful for control of arthropod pests.
    Type: Application
    Filed: September 30, 2010
    Publication date: August 2, 2012
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventor: Mitsuhiko Iwakoshi
  • TARGETING NAD BIOSYNTHESIS IN BACTERIAL PATHOGENS
    Publication number: 20120190708
    Abstract: The emergence of multidrug-resistant pathogens necessitates the search for new antibiotics acting on previously unexplored targets. Nicotinate mononucleotide adenylyltransferase of the NadD family, an essential enzyme of NAD biosynthesis in most bacteria, was selected as a target for structure-based inhibitor development. To this end, the inventors have identified small molecule compounds that inhibit bacterial target enzymes by interacting with a novel inhibitory binding site on the enzyme while having no effect on functionally equivalent human enzymes.
    Type: Application
    Filed: July 12, 2010
    Publication date: July 26, 2012
    Applicants: UNIVERSITY OF MARYLAND, BALTIMORE, The Board of Regents of the University of the University of Texas System, SANFORD-BURNHAM MEDICAL RESEARCH INSTITUTE
    Inventors: Alexander Mackerell, JR., Hong Zhang, Andrei Osterman, Rohit Kolhatkar
  • "The Use of a PAR-1 Antagonist in Combination with a P2Y12 ADP Receptor Antagonist for Inhibition of Thrombosis"
    Publication number: 20120184504
    Abstract: The treatment and prevention of thrombotic events are provided through co-administration of PAR-1 and the P2Y12 ADP receptor antagonists. Combined inhibition of the PAR-1 and the P2Y12 ADP platelet activation pathways had synergistic antithrombotic and antiplatelet effects, as demonstrated in co-administration of SCH 602539 and cangrelor.
    Type: Application
    Filed: September 24, 2010
    Publication date: July 19, 2012
    Inventors: John T. Strony, Madhu Chintala
  • THERAPEUTIC AGENT FOR MOOD DISORDERS
    Publication number: 20120184554
    Abstract: Provided are an agent for the treatment and/or prophylaxis of a mood disorder comprising, as an active ingredient, a thiazole derivative represented by the formula (I) wherein R1 represents aryl or the like, and R2 represents pyridyl or the like, or a pharmaceutically acceptable salt thereof, and the like.
    Type: Application
    Filed: September 2, 2010
    Publication date: July 19, 2012
    Applicant: Kyowa Hakko Kirin Co., Ltd.
    Inventors: Koji Yamada, Tomoyuki Kanda
  • RHO KINASE INHIBITORS
    Publication number: 20120178752
    Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1 and X are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Application
    Filed: June 29, 2011
    Publication date: July 12, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: John David GINN, Daniel Richard MARSHALL, Robert SIBLEY, Ronald John SORCEK, Erick Richard Roush YOUNG, Yunlong ZHANG
  • HETEROARYLS AND USES THEREOF
    Publication number: 20120178723
    Abstract: This invention provides compounds of formula IA-a or IB-a and subsets thereof: wherein Z, HY, R1, R2, G1, W, n, and A and subsets thereof are as described in the specification. The compounds are inhibitors of PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
    Type: Application
    Filed: August 11, 2011
    Publication date: July 12, 2012
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Masaaki Hirose, Zhigen Hu, Yongbo Hu, Hong Myung Lee, Zhan Shi, Stepan Vyskocil, Tianlin Xu
  • Medicaments for Inhibiting Thrombus Formation
    Publication number: 20120178777
    Abstract: A Medicaments for inhibiting thrombus formation contains active ingredients which are triflusal and clopidogrel bisulfate, wherein a mass ratio of triflusal to clopidogrel bisulfate is (100-650):(30-150), preferably (1-20):1, more preferably (3-6):1, and even more preferably 3:1 or 6:1.
    Type: Application
    Filed: March 17, 2010
    Publication date: July 12, 2012
    Applicant: Guizhou Liansheng Parmaceutical Co., Ltd.
    Inventor: Chunhua Su
  • CYCLOALKYL-HYDROXYL COMPOUNDS AND COMPOSITIONS FOR CHOLESTEROL MANAGEMENT AND RELATED USES
    Publication number: 20120172337
    Abstract: The present invention relates to novel cycloalkyl-hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, Syndrome X, thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient.
    Type: Application
    Filed: March 8, 2012
    Publication date: July 5, 2012
    Applicant: Esperion Therapeutics, Inc.
    Inventors: Jean-Louis Henri Dasseux, Carmen Daniela Oniciu
  • 5-amino-2-(1-hydroxy-ethyl)-tetrahydropyran derivatives
    Patent number: 8211890
    Abstract: The invention relates to antibacterial compounds of formula I wherein R1 represents alkoxy (notably methoxy); R2 represents H or F; each of R3, R4, R5 and R6 represents independently H or D; V represents CH and W represents CH or N, or V represents N and W represents CH; Y represents CH or N; Z represents O, S or CH2; and A represents CH2, CH2CH2 or CD2CD2; and salts of such compounds.
    Type: Grant
    Filed: December 11, 2009
    Date of Patent: July 3, 2012
    Assignee: Actelion Pharmaceuticals
    Inventors: Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn-Acklin
  • RHO KINASE INHIBITORS
    Publication number: 20120165322
    Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1 and R2 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Application
    Filed: June 29, 2011
    Publication date: June 28, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Brian Nicholas Cook, Jennifer A. Kowalski, Xiang Li, Daniel Richard Marshall, Sabine Schlyer, Robert Sibley, Lana Louise Smith-Keenan, Fariba Soleymanzadeh, Ronald John Sorcek, Erick Richard Roush Young, Yunlong Zhang
  • BICYCLIC AND TRICYCLIC DERIVATIVES AS THROMBIN RECEPTOR ANTAGONISTS
    Publication number: 20120157403
    Abstract: Heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salt or solvate of said compound, isomer or racemic mixture wherein represents an optional double bond, the dotted line is optionally a bond or no bond, resulting in a double bond or a single bond, as permitted by the valency requirement and wherein E, A, G M, Het, B, X, R3, R10, R11, R32 and R33 are herein defined and the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.
    Type: Application
    Filed: February 24, 2012
    Publication date: June 21, 2012
    Inventors: Samuel Chackalamannil, Mariappan V. Chelliah, Yuguang Wang, Yan Xia
  • 5-cyanothienopyridines for the treatment of tumours
    Patent number: 8202882
    Abstract: Novel 5-cyanothienopyridines of the formula (I), in which R1, R2 and R3 have the meanings indicated in claim 1, are inhibitors of TGF-beta receptor kinase, and can be employed, inter alia, for the treatment of tumors.
    Type: Grant
    Filed: September 19, 2008
    Date of Patent: June 19, 2012
    Assignee: Merck Patent Gesellschaft MIT Beschränkter Haftung
    Inventors: Guenter Hoelzemann, Ulrich Graedler, Hartmut Greiner, Christiane Amendt, Djordje Musil, Per Hillertz
  • PRASUGREL IN NON-CRYSTALLINE FORM AND PHARMACEUTICAL COMPOSITION THEREOF
    Publication number: 20120149727
    Abstract: The present invention relates to prasugrel or a pharmaceutically compatible salt thereof, compositions that contain this active substance and pharmaceutical compositions that contain this active substance or a composition containing this active substance. The present invention further relates to methods for producing the novel compositions.
    Type: Application
    Filed: August 4, 2010
    Publication date: June 14, 2012
    Inventors: Sandra Brueck, Jana Paetz
  • METHODS AND COMPOSITIONS USING RACEMIC, (R)-, AND (S)-FEXOFENADINE IN COMBINATION WITH LEUKOTRIENE INHIBITORS
    Publication number: 20120149730
    Abstract: Methods and pharmaceutical compositions employing a terfenadine metabolite and a leukotriene inhibitor for the treatment or prevention of inflammation or allergic disorders, such as asthma, or symptoms thereof. Also included are methods and compositions employing a terfenadine metabolite, a leukotriene inhibitor, and a decongestant for the treatment or prevention of inflammation or allergic disorders, such as asthma, or symptoms thereof.
    Type: Application
    Filed: February 16, 2012
    Publication date: June 14, 2012
    Inventor: Paul D. RUBIN
  • Crystal Forms of Kinase Inhibitors
    Publication number: 20120149726
    Abstract: N-(4-{4-amino-7-[1-(2-hydroxyethyl)-1H-pyrazol-4-yl]thieno[3,2-c]pyridin-3-yl}phenyl)-N?-(3-fluorophenyl)urea free base and crystallines form thereof are suitable pharmaceutical ingredients for pharmaceutical compositions useful in the treatment of disease, for example, cancer.
    Type: Application
    Filed: June 9, 2011
    Publication date: June 14, 2012
    Applicant: ABBOTT LABORATORIES
    Inventors: Geoff G. Z. Zhang, Paul J. Brackemeyer, Ahmad Y. Sheikh
  • Cycloalkylidene and heterocycloalkylidene inhibitor compounds
    Patent number: 8198299
    Abstract: The present invention provides a compound of general Formula (I) having histone deacetylase (HDAC) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.
    Type: Grant
    Filed: October 28, 2011
    Date of Patent: June 12, 2012
    Assignee: Gilead Sciences, Inc.
    Inventors: Lawrence S. Melvin, Jr., Michael Graupe, Chandrasekar Venkataramani, Juan A. Guerrero
  • THROMBIN RECEPTOR ANTAGONIST AND CLOPIDOGREL FIXED DOSE TABLET
    Publication number: 20120141586
    Abstract: The present invention provides for a pharmaceutical formulation which comprises a) a compound of the formula (I): SCH 530348 or the bisulfate salt thereof; b) clopidogrel; and c) silicified microcrystalline cellulose.
    Type: Application
    Filed: June 7, 2010
    Publication date: June 7, 2012
    Inventors: Rubi Burlage, Abdul S. Gafur, Srinivas S. Duggirala
  • Thieno[2 3-b]pyridines as potassium channel inhibitors
    Patent number: 8193215
    Abstract: The invention provides compounds of the formula: wherein R1 is aryl, heteroaryl, cycloalkyl or alkyl; R2 is H, alkyl, nitro, CO2R7, CONR5R6 or halo; R3 and R4 are H, NR5R6, NC(O)R7, halo, trifluromethyl, alkyl, CONR5R6, CO2R7, nitrile or alkoxy; R5 and R6 may be the same or different and may be H, alkyl, aryl, heteroaryl or cycloalkyl; or R5 and R6 may together form a saturated, unsaturated or partially saturated 4 to 7 member ring, wherein said ring may optionally comprise one or more further heteroatoms selected from N, O or S; R7 is H or alkyl; A is H, halo, or a group of formula X-L-Y; X is O, S or NR8; R8 is H or alkyl; L is (CH2)n, where n is 0, 1, 2, 3 or 4; and Y is aryl, a heterocyclic group, alkyl, alkenyl or cycloalkyl; the products of mono- and di-oxidation of sulphur and/or mono-oxidation of nitrogen moieties in compounds of formula I; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: August 18, 2009
    Date of Patent: June 5, 2012
    Assignee: Xention Limited
    Inventors: John Ford, Nicholas John Palmer, John Frederick Atherall, David John Madge, Derek John
  • GAMMA SECRETASE MODULATORS
    Publication number: 20120129846
    Abstract: In its many embodiments, the present invention provides a novel class of heterocyclic compounds of the formula: as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.
    Type: Application
    Filed: November 5, 2009
    Publication date: May 24, 2012
    Inventors: Zhaoning Zhu, William J. Greenlee, Mihir Baran Mandal, Duane A. Burnett, Chad E. Bennett, Troy McCracken
  • COMPOUNDS, COMPOSITIONS AND METHODS USEFUL FOR CHOLESTEROL MOBILISATION
    Publication number: 20120129856
    Abstract: The invention relates to classes of pharmaceutically-active heterocyclic compounds and pharmaceutically acceptable salts, and hydrates thereof, and compositions comprising the same. The invention also relates to methods for treating or preventing a disease or disorder, which comprises administering a therapeutically or prophylactically effective amount a compound described herein.
    Type: Application
    Filed: October 18, 2011
    Publication date: May 24, 2012
    Applicant: Cerenis Therapeutics SA
    Inventors: Daniela Carmen Oniciu, Jean-Louis Henri Dasseux, Ronald Barbaras, Valery Kochubey, Dmitry Kovalsky, Oleg Gennadievich Rodin, Otto Geoffroy, Anna Rzepiela
  • ANTIBACTERIAL AGENTS
    Publication number: 20120122918
    Abstract: Compounds of formula (1) have antibacterial activity: wherein R represents hydrogen or 1, 2 or 3 optional substituents; W is ?C(R1)—; R1 is hydrogen and R2 is hydrogen, methyl, or fluorine; or R1 and R2 taken together are —CH2—, —CH2CH2, —O—, or, in either orientation, —O—CH2— or —OCH2CH2—; and R3 is a radical of formula -(Alk1)m-(Z)p-(Alk2)-Q.
    Type: Application
    Filed: November 28, 2011
    Publication date: May 17, 2012
    Applicant: BIOTA SCIENTIFIC MANAGEMENT PTY LTD
    Inventors: David Ryall BROWN, Ian COLLINS, Lloyd George CZAPLEWSKI, David John HAYDON
  • Compositions for Treating Bacterial Infections
    Publication number: 20120122877
    Abstract: The present invention is antibiotic compositions having the ability to disrupt a MazEF complex in S. aureus. The compositions also have the ability to inhibit growth of S. aureus and as such are useful as antibiotic compounds.
    Type: Application
    Filed: July 1, 2010
    Publication date: May 17, 2012
    Applicant: TRUSTEES OF DARTMOUTH COLLEGE
    Inventors: Ambrose Cheung, Zhibiao Fu
  • Apoptosis signal-regulating kinase 1 inhibitors
    Patent number: 8178555
    Abstract: The present invention relates to apoptosis signal-regulating kinase 1 (“ASK1”) inhibiting compounds of the formula wherein the variables are as defined herein. The invention also relates to pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.
    Type: Grant
    Filed: June 23, 2009
    Date of Patent: May 15, 2012
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Edcon Chang, Stephen L. Gwaltney, Angie Vassar
  • PHARMACEUTICAL COMPOSITION HAVING IMPROVED SOLUBILITY
    Publication number: 20120114711
    Abstract: It is desired to provide a pharmaceutical composition containing a compound represented by formula (I) or a pharmacologically acceptable salt thereof, or a solvate thereof, which exhibits an inhibitory effect on activated blood coagulation factor X (FXa), and is useful as an agent for preventing and/or treating thrombosis, wherein the pharmaceutical composition exhibits favorable dissolution properties. The present invention relates to a solid pharmaceutical composition containing a compound represented by formula (I) or a pharmacologically acceptable salt thereof, or a solvate thereof, wherein the content of the compound represented by formula (I) is 0.5% by weight or more and less than 15% by weight with respect to the total weight of the pharmaceutical composition.
    Type: Application
    Filed: December 16, 2011
    Publication date: May 10, 2012
    Applicant: DAIICHI SANKYO COMPANY, LIMITED
    Inventors: Makoto Kamada, Motonori Kidokoro, Gaku Sekiguchi
  • Glucokinase activator
    Patent number: 8173649
    Abstract: A compound represented by the following formula (1): (wherein the carbon atom denoted by * is in the R-configuration; R1 and R2 are each independently a hydrogen atom, a halogen atom, an amino group, a hydroxyl group, a hydroxyamino group, a nitro group, a cyano group, a sulfamoyl group, a C1-C6 alkyl group, a C1-C6 alkoxy group, a C1-C6 alkylsulfanyl group, a C1-C6 alkylsulfinyl group or a C1-C6 alkylsulfonyl group; and A is a substituted or unsubstituted heteroaryl group), or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: December 21, 2007
    Date of Patent: May 8, 2012
    Assignees: Kyorin Pharmaceutical Co., Ltd., Teijin Pharma Limited
    Inventors: Yasumichi Fukuda, Yoshikazu Asahina, Ayako Nakamura, Kenji Fujita, Tomohiro Ide, Fumiyoshi Kobayashi, Shinji Kobayashi, Kanji Komatsu, Masanori Yamamoto
  • NEW THERAPEUTIC APPROACHES FOR TREATING NEUROINFLAMMATORY CONDITIONS
    Publication number: 20120108528
    Abstract: The present invention relates to novel compositions which can be used for the treatment of neuroinflammation, in particular in subjects having a neurodegenerative, autoimmune, infectious, toxic or traumatic disorder. More particularly, the invention relates to combined therapies for treating neuroinflammation. The invention also discloses new methods for treating neuroinflammation pathological conditions in a subject.
    Type: Application
    Filed: March 29, 2010
    Publication date: May 3, 2012
    Applicant: Pharnext
    Inventors: Daniel Cohen, Serguei Nabirochkin, Ilya Chumakov
  • FUSED PIPERIDINE COMPOUND AND PHARMACEUTICAL CONTAINING SAME
    Publication number: 20120108581
    Abstract: The present invention provides a low molecular weight compound having EPO production-promoting action and/or hemoglobin production-promoting action. The present invention relates to a fused piperidine compound represented by the following general formula (1): (wherein, ring A represents a C10-14 aryl group or 5- to 10-membered heterocyclic group, X represents N—R7, a sulfur atom or an oxygen atom, R1, R2, R2?, R3 and R3? independently represent a hydrogen atom, C1-6 alkyl group or C3-6 cycloalkyl group, and R4, R5 and R6 independently represent a hydrogen atom or halogen atom), or a salt thereof, or a solvate thereof.
    Type: Application
    Filed: March 25, 2010
    Publication date: May 3, 2012
    Applicant: Kowa Company, Ltd
    Inventors: Masanori Ashikawa, Toshiharu Morimoto, Hajime Yamada, Shunji Takemura, Tatsuaki Nishiyama, Takeshi Doi, Hiroyuki Ishiwata
  • INHIBITORS OF PROTEIN TYROSINE KINASE ACTIVITY
    Publication number: 20120108628
    Abstract: This invention relates to compounds that inhibit protein tyrosine kinase activity. In particular the invention relates to compounds that inhibit the protein tyrosine kinase activity of growth factor receptors, resulting in the inhibition of receptor signaling, for example, the inhibition of VEGF receptor signaling and HGF receptor signaling. More particularly, the invention relates to compounds, compositions and methods for the inhibition of VEGF receptor signaling and HGF receptor signaling. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.
    Type: Application
    Filed: December 30, 2011
    Publication date: May 3, 2012
    Inventors: Stephen William Claridge, Ljubomir Isakovic, Michael Mannion, Stephane Raeppel, Oscar Mario Saavedra, Frédéric Gaudette, Lijie Zhan, Arkadii Vaisburg
  • THERAPEUTIC AGENT FOR MOTOR DISORDERS
    Publication number: 20120101101
    Abstract: Provided are an agent for the treatment and/or prophylaxis of a movement disorder, the agent for the treatment and/or prophylaxis wherein the movement disorder is extrapyramidal syndrome, the agent for the treatment and/or prophylaxis wherein the movement disorder is bradykinesia, gait disturbance, dystonia, dyskinesia or tardive dyskinesia, the agent for the treatment and/or prophylaxis wherein the movement disorder is a side effect of L-DOPA and/or dopamine agonist therapy, and the like, each containing a thiazole derivative represented by the formula (I) wherein R1 represents aryl and the like, and R2 represents pyridyl or the like, or a pharmaceutically acceptable salt thereof as an active ingredient.
    Type: Application
    Filed: April 28, 2010
    Publication date: April 26, 2012
    Applicant: KYOWA HAKKO KIRIN CO., LTD.
    Inventors: Noriaki Uesaka, Takashi Sawada, Tomoyuki Kanda
  • TGF-Beta Stimulating Agent Compositions and Combinations
    Publication number: 20120100204
    Abstract: Compositions and methods for preventing, inhibiting or treating a disorder associated with the loss of normal adult tissue architecture are provided.
    Type: Application
    Filed: October 25, 2011
    Publication date: April 26, 2012
    Applicant: TCP INNOVATIONS LTD
    Inventor: David J. Grainger
  • Benzoxathiin derivative
    Patent number: 8163770
    Abstract: Disclosed is a compound represented by the formula (I) below and a pharmaceutically acceptable salt thereof. This compound is useful for treatment of obesity, diabetes and the like. [In the formula (I), Ar represents a benzene ring or the like; X1 represents a nitrogen atom, a sulfur atom or the like; R1 represents an aryl group or the like; X2 represents a group represented by the following formula (II): (wherein R4 and R5 respectively represent a lower alkyl group or the like, and m represents a number of 2-4) or the like; one of X and Y represents an oxygen atom and the other represents a sulfanyl group or the like; and X3-X6 respectively represent —CH—, a nitrogen atom or the like.
    Type: Grant
    Filed: October 25, 2006
    Date of Patent: April 24, 2012
    Assignee: MSD. K. K.
    Inventors: Takashi Mizutani, Nagaaki Sato, Takahide Sasaki, Toshiyuki Takahashi
  • Amide derivatives as ion-channel ligands and pharmaceutical compositions and methods of using the same
    Patent number: 8163901
    Abstract: Compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.
    Type: Grant
    Filed: January 9, 2009
    Date of Patent: April 24, 2012
    Assignee: Evotec AG
    Inventors: Matthew Duncton, Donogh John Roger O'Mahony, Matthew Cox, Maria De Los Angeles Estiarte-Martinez
  • METNASE AND INTNASE INHIBITORS AND THEIR USE IN TREATING CANCER
    Publication number: 20120093917
    Abstract: This invention relates to novel cancer treatment compositions and associated therapeutic methods. More particularly, this invention relates in part to small chemical inhibitors of DNA repair proteins (Metnase) and to a therapeutic method that utilizes the inhibitors to increase the effectiveness of cancer treatment protocols.
    Type: Application
    Filed: March 31, 2010
    Publication date: April 19, 2012
    Inventors: Robert Hromas, Andrei Leitao, Tudor I. Oprea, Larry A. Sklar, Elizabeth A. Williamson, Justin Wray
  • CRYSTALS OF PRASUGREL HYDROBROMATE
    Publication number: 20120095035
    Abstract: The present application discloses crystals of 2-acetoxy-5-(?-cyclopropylcarbonyl-2-fluorobenzyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine hydrobromate, crystal compositions and pharmaceutical compositions comprising them and their use. The crystals of prasugrel hydrobromate of the present application possess excellent stability and solubility.
    Type: Application
    Filed: March 31, 2010
    Publication date: April 19, 2012
    Applicants: NANJING CHIA TAI TIANQING PHARMACEUTICAL CO., LTD., SHANGHAI INSTITUTE OF PHARMACEUTICAL INDUSTRY
    Inventors: Zhedong Yuan, Xingdong Cheng, Yulei Yang, Ling Tong, Xiong Yu, Laifang Zhang, Wenliang Zhou
  • FUSED HETEROCYCLIC COMPOUNDS AND THEIR USES
    Publication number: 20120088766
    Abstract: The present application relates to therapeutic organic compounds, compositions comprising an effective amount of a therapeutic organic compound; and methods for treating and preventing disease comprising administering and effective amount of a therapeutic organic compound to a subject in need thereof.
    Type: Application
    Filed: June 14, 2010
    Publication date: April 12, 2012
    Applicant: DANA-FARBER CANCER INSTITUTE, INC.
    Inventors: Hwan Geun Choi, Taebo Sim, Nathanael Gray, Wenjun Zhou, Jae Won Chang, Jianming Zhang, Ellen Weisberg
  • INHIBITORS OF VEGF RECEPTOR AND HGF RECEPTOR SIGNALING
    Publication number: 20120083482
    Abstract: The invention relates to the inhibition of VEGF receptor signaling and HGF receptor signaling. The invention provides compounds of general formula (A) wherein A1 is sulfur, A3 is CH, A2 is CH, D is heterocycle, Z is oxygen, SO0-2 or NR, Ar is phenyl and G is not a ring, and methods for inhibiting VEGF receptor signaling and HGF receptor signaling. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.
    Type: Application
    Filed: December 8, 2011
    Publication date: April 5, 2012
    Inventors: Oscar Mario Saavedra, Stephen William Claridge, Lijie Zhan, Franck Raeppel, Arkadii Vaisburg, Stephane Raeppel, Michael Mannion, Frederic Gaudette, Ljubomir Isakovic, Marie-Claude Granger, Naomy Bernstein
  • Novel Therapeutic Treatments Using Centhaquin
    Publication number: 20120083447
    Abstract: Methods of treating hypertension, pain, and resuscitative hemorrhagic shock using an adrenergic agent, like centhaquin, are disclosed. The methods treat mammals, including humans.
    Type: Application
    Filed: April 29, 2010
    Publication date: April 5, 2012
    Applicant: MIDWESTERN UNIVERSITY
    Inventor: Anil Gulati
  • METHOD AND COMPOSITION USING A DUAL SPECIFICITY PROTEIN TYROSINE PHOSPHATASE AS AN ANTIMALARIAL DRUG TARGET
    Publication number: 20120077869
    Abstract: Phosphotyrosine phosphatase (PTP) encoded by PF13_0027 is a desirable drug target for the human malaria parasite Plasmodium falciparum. This PTP is critical for intraerythrocytic parasite development and invasion of erythrocytes by malaria merozoites. Mutation of the PF13_0027 gene or blocking expression of PTP function to create a PTP-null parasite severely attenuates the malaria parasite's ability to survive, making the PTP-null parasite suitable as an attenuated blood-stage parasite vaccine.
    Type: Application
    Filed: September 20, 2011
    Publication date: March 29, 2012
    Applicant: UNIVERSITY OF SOUTH FLORIDA
    Inventors: John H. Adams, Bharath Balu, Steven P. Maher, Christopher O. Campbell, Roman Manetsch
  • METHOD OF TREATING CANCER WITH SUBSTITUTED AMIDE DERIVATIVES
    Publication number: 20120070413
    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: Application
    Filed: November 30, 2011
    Publication date: March 22, 2012
    Inventors: Tae-Seong KIM, David Bauer, Steven Bellon, Alessadro Boezio, Shon Booker, Deborah Choquette, Derin C. D'Amico, Noel D'Angelo, Celia Dominguez, Ingrid M. Fellows, Julie Germain, Russell Graceffa, Jean-Christophe Harmange, Satoko Hirai, Daniel La, Matthew Lee, Longbin Liu, Mark H. Norman, Michele Potashman, Philip Roveto, Aaron C. Siegmund, Ning Xi, Kevin Yang
  • Method and Composition for Treating Diabetic Ketoacidosis
    Publication number: 20120070513
    Abstract: Methods of treating diabetic ketoacidosis are disclosed. The methods utilize an endothelin antagonist to treat diabetic ketoacidosis in mammals, including humans.
    Type: Application
    Filed: April 30, 2010
    Publication date: March 22, 2012
    Inventor: Anil Gulati
  • UREA DERIVATIVES HAVING PI3K-INHIBITING ACTIVITY
    Publication number: 20120071475
    Abstract: Provided is a compound or a pharmaceutically acceptable salt thereof which inhibits the activity of PI3K to regulate many biological processes including the growth, differentiation, survival, proliferation, migration, metabolism, and the like of cells and is therefore useful for the prophylaxis/therapy of diseases including inflammatory diseases, arteriosclerosis, vascular/circulatory diseases, cancer/tumors, immune system diseases, cell proliferative diseases, infectious diseases, and the like. The above problem was solved by providing a urea derivative shown in the present specification, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: April 26, 2010
    Publication date: March 22, 2012
    Applicant: SHIONOGI & CO., LTD.
    Inventors: Daisuke Taniyama, Yasunori Mitsuoka, Kayoko Hata
  • THERAPEUTIC APPROACHES FOR TREATING ALZHEIMER DISEASE AND RELATED DISORDERS THROUGH A MODULATION OF ANGIOGENESIS
    Publication number: 20120058992
    Abstract: The present invention relates to compositions and methods for the treatment of Alzheimer's disease and related disorders. More particularly, the invention relates to combined therapies that modulate angiogenesis for treating said disease.
    Type: Application
    Filed: October 29, 2010
    Publication date: March 8, 2012
    Applicant: PHARNEXT
    Inventors: Daniel Cohen, Ilya Chumakov, Serguei Nabirochkin, Oxana Guerassimenko, Esther Graudens
  • METHODS FOR THE TREATMENT OR PROPHYLAXIS OF THROMBOSIS OR EMBOLISM
    Publication number: 20120053157
    Abstract: The present invention relates to a method of ameliorating the drawbacks of anti-platelet drug named clopidogrel. The method of the present invention comprises administration of an (S)oxo-clopidogrel or its derivative of the Formula IIA in its free or pharmaceutically acceptable salt form for alleviating the symptoms of thrombosis or embolism by inhibiting blood platelet aggregation. Compositions for use in such methods are also provided.
    Type: Application
    Filed: August 26, 2011
    Publication date: March 1, 2012
    Applicant: IPCA LABORATORIES LIMITED
    Inventors: Ashok Kumar, Nellithanath Thankachen Byju
  • METHOD OF TREATING THROMBOCYTOPENIA
    Publication number: 20120052055
    Abstract: Invented is a method of treating thrombocytopenia in a human, in need thereof which comprises the in vivo administration of a therapeutically effective amount of a peptide or a non-peptide TPO receptor agonist and an anti-clotting agent or agents, and optional further active ingredients, to such human.
    Type: Application
    Filed: May 6, 2010
    Publication date: March 1, 2012
    Applicant: Glaxosmithkline LLC
    Inventors: Connie L. Erickson-Miller, Michael Arning