Ring Sulfur In The Bicyclo Ring System Patents (Class 546/114)
  • MCH receptor antagonists
    Patent number: 8263772
    Abstract: The present invention relates to a melanin concentrating hormone antagonist compound of formula (1): wherein R1, Ra, Rb, R2, L1, R3, R4 and R5 are as defined, or a pharmaceutically acceptable salt, enantiomer, diastereomer or mixture of diasteromers thereof useful in the treatment, obesity and related diseases.
    Type: Grant
    Filed: June 8, 2007
    Date of Patent: September 11, 2012
    Assignee: Eli Lilly and Company
    Inventors: Macklin Brian Arnold, Yen Dao, Kevin Matthew Gardinier, David Joseph Garmene, Steven James Green, Erik James Hembre, Jianliang Lu
  • Thieno [2,3-b] pyridine compounds with mGluR activity
    Patent number: 8263773
    Abstract: Provided herein are Thieno[2,3-b]pyridine compounds with mGluR activity. Also provided herein are processes and intermediates for the preparation of the Thieno[2,3-b]pyridine compounds, pharmaceutical compositions containing these compounds, and the use of these compounds in treatment, therapy, and/or prevention of conditions which require modulation of mGluR1 and mGluR5 receptors.
    Type: Grant
    Filed: June 24, 2009
    Date of Patent: September 11, 2012
    Assignee: Richter Gedeon Nyrt.
    Inventors: Istvan Gyertyan, Katalin Nogradi, Ottilia Elekes, Monika Vastag, Amrita Agnes Bobok, Katalin Saghy
  • MST1 KINASE INHIBITORS AND METHODS OF THEIR USE
    Publication number: 20120225857
    Abstract: Compounds for the inhibition of mammalian Ste20-like kinase 1 (MST1) are disclosed, along with compositions comprising them and methods of their use in the treatment, management or prevention of an inflammatory or autoimmune diseases or disorders.
    Type: Application
    Filed: March 2, 2012
    Publication date: September 6, 2012
    Inventors: David John Augeri, Jeffrey Thomas Bagdanoff, Simon David Peter Baugh, Marianne Carlsen, Kenneth Gordon Carson, John Anthony Gilleran, Wei He, Tamas Oravecz, Konstantin Salojin, Leonard Sung
  • Glucokinase Activators
    Publication number: 20120225887
    Abstract: Compounds are provided for use with glucokinase that comprise the formula: wherein the variables are as defined herein. Also provided are 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: Application
    Filed: April 10, 2012
    Publication date: September 6, 2012
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Zacharia Cheruvallath, Stephen L. Gwaltney, Andrew John Jennings, Mark Sabat, Jeffrey A. Stafford, Mingnam Tang, Haxia Wang
  • FUSED HETEROCYCLIC RING DERIVATIVE AND USE THEREOF
    Publication number: 20120220569
    Abstract: The present invention provides a fused heterocycle derivative having a strong Smo inhibitory activity, and use thereof. Specially, the present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or salt thereof, and a medicament containing the compound or a prodrug thereof, which is an Smo inhibitor or an agent for the prophylaxis or treatment of cancer.
    Type: Application
    Filed: August 25, 2010
    Publication date: August 30, 2012
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Tomohiro Ohashi, Zenyu Shiokawa, Yuta Tanaka, Satoshi Sasaki
  • Thiazolo[5,4-B]pyridine glucokinase activators
    Patent number: 8252931
    Abstract: The present invention provides compounds of the formula which are activators of glucokinase activity and, thus, may be employed as therapeutic agents for the treatment of glucokinase mediated conditions. Accordingly, the compounds of formula (I) may be employed for the prevention and the treatment of impaired glucose tolerance, type 2 diabetes and obesity.
    Type: Grant
    Filed: September 28, 2006
    Date of Patent: August 28, 2012
    Assignee: Novartis AG
    Inventors: Gregory Raymond Bebernitz, Louise Kirman
  • ACETAMIDE DERIVATIVES AS GLUCOKINASE ACTIVATORS, THEIR PROCESS AND MEDICINAL APPLICATIONS
    Publication number: 20120214735
    Abstract: Acetamide derivatives, their stereoisomers, tautomers, prodrugs, pharmaceutically acceptable salts, polymorphs, solvates and formulations thereof for the prophylaxis, management, treatment, control of progression, or adjunct treatment of diseases and/or medical conditions where the activation of glucokinase would be beneficial, are disclosed. The disclosure also provides process of preparation of these acetamide derivatives.
    Type: Application
    Filed: February 17, 2012
    Publication date: August 23, 2012
    Applicant: Advinus Therapeutics Limited
    Inventors: Debnath Bhuniya, Anil Deshpande, Sachin Kandalkar, Balasaheb Kobal, Santosh Kurhade, Vinod Vyavahare, Rahul Kaduskar
  • IAP inhibitors
    Patent number: 8247557
    Abstract: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula (I): wherein Q, X1, X2, Y, Z1, Z2, Z3, Z4, R1, R2, R3, R3?, R4, R4?, R5, R6, R6? and n are as described herein.
    Type: Grant
    Filed: December 19, 2006
    Date of Patent: August 21, 2012
    Assignee: Genentech, Inc.
    Inventors: Michael F. T. Koehler, Lewis Gazzard, Vickie Hsiao-Wei Tsui
  • Process for the preparation of clopidogrel and its pharmaceutically acceptable salts
    Patent number: 8247558
    Abstract: The present invention provides a process for the preparation of clopidogrel and its pharmaceutically acceptable salts thereof comprises the resolving racemic methyl alpha-5-(4,5,6,7-tetrahydro[3,2-c]thienopyridyl)(2-chlorophenyl)-acetate by the salt formation of methyl alpha-5-(4,5,6,7-tetrahydro[3,2-c]thienopyridyl)(2-chlorophenyl)-acetate with excess levorotatory camphor-10-sulfonic acid to get a maximum yield of camphor sulphonate salt of methyl S-(+)-alpha-5-(4,5,6,7-tetrahydro[3,2-c]thienopyridyl) (2-chlorophenyl)-acetate and transforming the camphor sulphonate salt to clopidogrel or its pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: September 4, 2007
    Date of Patent: August 21, 2012
    Assignee: Ranbaxy Laboratories Limited
    Inventors: Parendn Dhirajlal Rathod, Satish Kumar Aryan, Ram Chander Aryan, Chandra Has Khanduri
  • 3-CARBAMOYL-2-PYRIDONE DERIVATIVES
    Publication number: 20120208813
    Abstract: The present invention provides compounds having an agonistic activity to the cannabinoid receptor, which is represented by the formula (I): wherein R1, R2, R3, R4, and G are defined as herein, a pharmaceutically acceptable salt or a solvate thereof, and pharmaceutical compositions, atopic dermatitis treating agents, and anti-pruritus agents, especially anti-pruritus agents for oral used and for external application, which each contains the said compound as an active ingredient.
    Type: Application
    Filed: February 28, 2012
    Publication date: August 16, 2012
    Inventors: Natsuki ISHIZUKA, Takashi SASATANI, Yoshiharu HIRAMATSU, Masanao INAGAKI, Masahide ODAN, Hiroshi HASHIZUMI, Susumu MITSUMORI, Yasuhiko FUJII, Yoshikazu FUKUI, Hideaki WATANABE, Jun SATO
  • 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
  • Crystalline Forms of Kinase Inhibitors
    Publication number: 20120203002
    Abstract: 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, Paul J. Brackemeyer, Ahmad Y. Sheikh
  • 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
  • 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
  • Processes For Preparing Prasugrel And Pharmaceutically Acceptable Salts Thereof
    Publication number: 20120202066
    Abstract: Disclosed are improved processes for preparing prasugrel compound of formula-(1), its intermediates and pharmaceutically acceptable salts.
    Type: Application
    Filed: October 7, 2010
    Publication date: August 9, 2012
    Inventors: Manne Satyanarayana Reddy, Srinivasan Thirumalai Rajan, Sajja Eswaraiah, Karamala Rama Subba Reddy, Bairy Kondal Reddy, Ghojala Venkat Reddy
  • 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
  • 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
  • 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
  • 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
  • Fused heterocyclic derivative and use thereof
    Patent number: 8217176
    Abstract: The present invention provides a compound having a superior Smo inhibitory activity and lower toxicity, which is sufficiently satisfactory as a pharmaceutical product. The present invention provides a compound represented by the formula wherein ring A is 5- to 7-membered ring optionally having substituent(s), where substituents are optionally bonded to each other to form a ring; X is O, S or NR1 (R1 is a hydrogen atom or a hydrocarbon group optionally having substituent(s)); R2 is carbamoyl optionally having substituent(s); and R3 is hydroxy optionally having substituent(s), or a salt thereof.
    Type: Grant
    Filed: February 25, 2009
    Date of Patent: July 10, 2012
    Assignee: Takeda Pharmaceutical Company Limited
    Inventor: Yuya Oguro
  • 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
  • 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
  • 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
  • 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
  • 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
  • METHOD FOR PREPARING PRASUGREL
    Publication number: 20120142927
    Abstract: The present invention relates to a method for synthesizing prasugrel, comprising, the following steps: converting o-fluorobenzyl cyclopropyl ketone into ?-cyclopropylcarbonyl-2-fluorobenzyl halide (compound 2) using dibromohydantoinhydantoin as halogenation reagent and acetic acid as solvent, then 2-oxo-4,5,6,7-tetrahydrothieno[3,2-c]pyridine p-toluenesulfonate (compound 4) is obtained with high yield by a concerted catalysis using a phase transfer catalyst and an inorganic salt, then is condensed and acylated to obtain prasugrel as a gum. The present invention also provides a method for purifying prasugrel comprising crystallizing using alcohols as a crystallization solvent to obtain prasugrel crystals with a high purity.
    Type: Application
    Filed: June 23, 2010
    Publication date: June 7, 2012
    Applicant: Zhejiang Huahai Pharmaceutical co., Ltd.
    Inventors: Chuangwei Liu, Qifeng Lu, Changhui Chen
  • Process for producing high-purity prasugrel and acid addition salt thereof
    Patent number: 8193358
    Abstract: The present invention is directed to providing prasugrel hydrochloride or the like with a reduced content of OXTP. A method for producing prasugrel hydrochloride with a reduced content of OXTP, comprising dissolving free prasugrel containing OXTP in an inert solvent and adding hydrochloric acid optionally dropwise to the solution for reaction is also provided.
    Type: Grant
    Filed: April 6, 2007
    Date of Patent: June 5, 2012
    Assignees: Daiichi Sankyo Company, Limited, Ube Industries, Ltd.
    Inventors: Masahiko Hagihara, Hiroyuki Miyata, Yukinori Wada, Naoyuki Yokota
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • PROCESSES AND INTERMEDIATES FOR PREPARING FUSED HETEROCYCLIC KINASE INHIBITORS
    Publication number: 20120095234
    Abstract: This invention relates to processes and intermediates for manufacturing fused heterocyclic-type kinase inhibitor compounds, such as thienopyridine-based compounds, and to processes and intermediates for preparing intermediates that are useful in the manufacture of fused heterocyclic-type kinase inhibitor compounds, such as thienopyridine-based compounds, particularly at an industrial level.
    Type: Application
    Filed: December 20, 2011
    Publication date: April 19, 2012
    Inventors: Franck Raeppel, Ljubomir Isakovic, Stephen William Claridge, Michael Mannion, Lijie Zhan, Marie-Claude Granger, Arkadii Vaisburg, Miguel Nantel
  • 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
  • Heterocyclic compounds, their preparation and their use as medicaments, in particular as anti-bacterial agents
    Patent number: 8148540
    Abstract: The invention relates to new heterocyclic compounds of general formula (I), and their salts with a base or an acid: The invention also relates to a process for the preparation of these compounds as well as their use as medicaments, in particular as anti-bacterial agents.
    Type: Grant
    Filed: June 7, 2007
    Date of Patent: April 3, 2012
    Assignee: AstraZeneca
    Inventors: Joseph Aszodi, Maxime Lampilas, Branislav Musicki, David Alan Rowlands, Pascal Colette
  • METHOD FOR PRODUCING A SOLID PREPARATION
    Publication number: 20120077980
    Abstract: A method for producing a solid preparation containing a compound represented by the formula (I) below or a pharmacologically acceptable salt thereof, which includes a step wherein a composition containing the compound represented by the formula (I) below or a pharmacologically acceptable salt thereof is mixed, while applying a mechanical stress to the composition. The compound of the formula (I) is as follows: The method results in improved dissolvability of the compound of the formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: December 7, 2011
    Publication date: March 29, 2012
    Applicants: UBE INDUSTRIES, LTD., DAIICHI SANKYO COMPANY, LIMITED
    Inventor: Tomoyuki WATANABE
  • 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
  • HERBICIDALLY ACTIVE KETOSULTAMS AND DIKETOPYRIDINES
    Publication number: 20120058893
    Abstract: Ketosultams and diketopyridines of the formula (I) and use thereof as herbicides are described. In this formula (I), G, X, Y and Z are each radicals such as hydrogen and organic radicals such as alkyl. W represents organic radicals such as alkyl. A represents a heterocycle.
    Type: Application
    Filed: August 31, 2011
    Publication date: March 8, 2012
    Applicant: BAYER CROPSCIENCE AG
    Inventors: Stefan LEHR, Christian WALDRAFF, Elmar GATZWEILER, Isolde HÄUSER-HAHN, Ines HEINEMANN, Christopher Hugh ROSINGER
  • OXAMIDE DERIVATIVE
    Publication number: 20120053349
    Abstract: The present invention provides an isomer of N1-(5-chloropyridin-2-yl)-N2-((1S,2R,4S)-4-[(dimethylamino)carbonyl]-2-{[(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridin-2-yl)carbonyl]amino}cyclohexyl)ethanediamide represented by formula (II) or a salt thereof, or a solvate thereof. Such an isomer or a salt thereof, or a solvate thereof is useful as a standard in a test for inspecting impurities in a pharmaceutical composition containing a compound represented by formula (II) or a salt thereof, or a hydrate thereof. The present invention also relates to a substantially pure compound that is useful as a preventive and/or therapeutic drug for thrombotic diseases, and a pharmaceutical composition containing the substantially pure compound.
    Type: Application
    Filed: October 14, 2011
    Publication date: March 1, 2012
    Applicant: DAIICHI SANKYO COMPANY, LIMITED
    Inventors: Toshiharu Yoshino, Yumi Nakamoto, Tomoyuki Nagai, Seishiro Uchida
  • Bicyclic PPAT inhibitors as antibacterial agents
    Patent number: 8124616
    Abstract: Disclosed are compounds of Formula I, pharmaceutical compositions comprising Formula I and methods of treating bacterial infections. The disclosed compounds are inhibitors of PPAT (phosphopantetheine adenyl transferase), and are useful in the treatment and prevention of diseases caused by bacteria, particularly bacteria dependent on PPAT, for example, species such Escherichia coli, Helicobacter pylori, Staphyloccocus aureus, and the like.
    Type: Grant
    Filed: November 26, 2008
    Date of Patent: February 28, 2012
    Assignee: Biota Scientific Management Pty Ltd
    Inventor: Roger Frechette
  • 7-AMINOFUROPYRIDINE DERIVATIVES
    Publication number: 20120046267
    Abstract: Compounds of Formula 1, as shown below and defined herein: pharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including treatment of cancers, such as tumors driven at least in part by TAK1 or for which an appropriate TAK1 inhibitor is effective. This Abstract is not limiting of the invention.
    Type: Application
    Filed: February 11, 2011
    Publication date: February 23, 2012
    Inventors: Keith R. Hornberger, Dan M. Berger, Xin Chen, Andrew P. Crew, Hanqing Dong, Andrew Kleinberg, An-Hu Li, Lifu Ma, Mark J. Mulvihill, Bijoy Panicker, Kam W. Siu, Arno G. Steinig, James G. Tarrant, Jing Wang, Qinghua Weng, Rajaram Sangem, Ramesh C. Gupta
  • CYCLOALKYLIDENE AND HETEROCYCLOALKYLIDENE INHIBITOR COMPOUNDS
    Publication number: 20120045412
    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: Application
    Filed: October 28, 2011
    Publication date: February 23, 2012
    Applicant: Gilead Sciences, Inc.
    Inventors: Lawrence S. Melvin, JR., Michael Graupe, Chandrasekar Venkataramani, Juan A. Guerrero
  • Diazabicyclic central nervous system active agents
    Patent number: 8119635
    Abstract: Compounds of formula I pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals.
    Type: Grant
    Filed: August 19, 2009
    Date of Patent: February 21, 2012
    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. Frost, Kevin B. Sippy