Chalcogen Bonded Directly To Ring Carbon Of Pyridine Or Partially Hydrogenated Pyridine Ring Patents (Class 546/261)
-
Publication number: 20120214253Abstract: The present invention provides a novel class of macrocyclic compounds as well as complexes formed between a metal (e.g., lanthanide) ion and the compounds of the invention. Preferred complexes exhibit high stability as well as high quantum yields of lanthanide ion luminescence in aqueous media without the need for secondary activating agents. Preferred compounds comprise hydroxypyridinonyl moieties within their macrocyclic structure and are characterized by surprisingly low, non-specific binding to a variety of polypeptides such as antibodies and proteins as well as high kinetic stability.Type: ApplicationFiled: August 24, 2010Publication date: August 23, 2012Applicant: LUMIPHORE, INC.Inventors: Nathaniel G. Butlin, Kenneth N. Raymond, Jide Xu, Anthony D'Aleo
-
Publication number: 20120208850Abstract: The invention relates to methods, compounds, and compositions for delivering 1,3-propanedisulfonic acid (1,3PDS) in a subject, preferably a human subject. The invention encompasses compounds that will yield or generate 1,3PDS, either in vitro or in vivo. The invention also relates to sulfonate ester prodrugs of 1,3PDS as well as Gemini dimmers and oligomers of 1,3PDS for the prevention or treatment of associated diseases and conditions.Type: ApplicationFiled: August 6, 2010Publication date: August 16, 2012Applicant: BELLUS HEALTH INC.Inventors: Xianqi Kong, Nigel Levens, Abderrahim Bouzide, Stephane Ciblat, Richard Frenette, Johanne Renaud
-
Patent number: 8242140Abstract: Compounds of formula I: wherein X, R2, R3, R5 and R6 are defined herein, are useful as inhibitors of the hepatitis C virus NS5B polymerase.Type: GrantFiled: July 31, 2008Date of Patent: August 14, 2012Assignee: Boehringer Ingelheim International GmbHInventors: Pierre L. Beaulieu, Paul J. Edwards, Martin Poirier, Jean Rancourt, Timothy A. Stammers
-
Publication number: 20120201816Abstract: 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: ApplicationFiled: April 12, 2012Publication date: August 9, 2012Applicant: BRISTOL-MYERS SQUIBB COMPANYInventors: 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
-
Publication number: 20120196901Abstract: The present invention is directed to tertiary amide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. 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 orexin receptors are involved.Type: ApplicationFiled: October 22, 2010Publication date: August 2, 2012Applicant: Merck Sharp & Dohme Corp.Inventors: Paul J. Coleman, Swati P. Mercer, Anthony J. Roecker
-
Publication number: 20120190852Abstract: The present invention is to provide a medical composition for the treatment or prophylaxis of glaucoma which comprises a pyridylaminoacetic acid compound represented by the formula (1): wherein R1, R2 and R3 each independently represent a hydrogen atom or C1-C6 alkyl group, Y represents a bicyclic heteroaromatic ring group which may be substituted by a group(s) selected from the group consisting of a halogen atom, C1-C6 alkyl group, halogeno C1-C6 alkyl group, C1-C6 alkoxyl group, halogeno C1-C6 alkoxyl group and C1-C6 alkylthio group or a group -Q1-Q2 wherein Q1 represents an arylene group or 5- to 6-membered heteroarylene group, Q2 represents an aromatic group or a 5- to 6-membered ring heterocyclic group each of which may be substituted by a group(s) selected from the group consisting of a halogen atom, hydroxyl group, C1-C6 alkyl group, halogeno C1-C6 alkyl group, C1-C6 alkoxyl group and halogeno C1-C6 alkoxyl group, Z represents an aromatic group or a 5- to 6-membered heteroaromatic ring group eaType: ApplicationFiled: March 30, 2010Publication date: July 26, 2012Applicant: UBE INDUSTRIES, LTD.Inventors: Masahiko Hagihara, Kenji Yoneda, Eiji Okanari, Manabu Shigetomi
-
Publication number: 20120190699Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing the compounds of the invention and intermediate compounds useful in these processes.Type: ApplicationFiled: December 14, 2011Publication date: July 26, 2012Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Jean-Damien Charrier, Steven Durrant, Sharn Ramaya, Juan-Miguel Jimenez, Alistair Rutherford
-
Publication number: 20120184747Abstract: This is to provide a novel aniline compound represented by the following formula (I) having an excellent broncho dilatory action based on potent EP2 agonistic action. A compound represented by the formula (I): or a salt thereof.Type: ApplicationFiled: September 10, 2010Publication date: July 19, 2012Applicant: UBE INDUSTRIES, LTD.Inventors: Ryo Iwamura, Yoko Murakami, Masahiko Hagihara, Eiji Okanari
-
Patent number: 8217173Abstract: Chelating monomers and fluoride-releasing compositions are disclosed that may be incorporated into dental composite restorative materials, dental bonding agents or other dental materials, to produce materials with high fluoride release rates, and high fluoride recharge capability. Such dental restorative materials may help reduce the level of dental caries in patients, particularly the level of caries occurring on the margins of the restorative materials.Type: GrantFiled: February 12, 2008Date of Patent: July 10, 2012Assignee: Board of Supervisors of Louisiana State University and Agricultural and Mechanical CollegeInventors: Xiaoming Xu, Shailaja Jayaramachandran, Liang Chen
-
Publication number: 20120165339Abstract: A cyclopropane derivative represented by the following formula (I) or a pharmaceutically acceptable salt thereof has orexin receptor inhibitory action, and thus, is extremely useful as an agent for preventing or treating sleep disorder or dyssomnia caused by orexin, including insomnia as a typical example: wherein A1, A2 and A3 each independently represent an aryl group, a heterocyclyl group or the like, R1, R2 and R3 each independently represent a hydrogen atom, a C1-6 alkyl group or the like, X represents an oxygen atom or the like, and L represents a bond or the like.Type: ApplicationFiled: December 20, 2011Publication date: June 28, 2012Applicant: EISAI R&D MANAGEMENT CO., LTD.Inventors: Taro Terauchi, Ayumi Takemura, Yuji Kazuta, Fumihiro Ozaki, Takashi Doko, Yu Yoshida, Toshiaki Tanaka, Keiichi Sorimachi, Yoshimitsu Naoe, Carsten Beuckmann
-
Publication number: 20120157681Abstract: There is described novel organo-platinum luminophores comprising a complex of formula I: The luminophores have application as the emissive component in organic light emitting diodes.Type: ApplicationFiled: December 16, 2011Publication date: June 21, 2012Applicant: UNIVERSITY OF YORKInventors: Duncan W. Bruce, Valery Kozhevnikov
-
Patent number: 8202997Abstract: A method for treating or preventing injury of a biological material exposed to hypoxic or ischemic conditions comprising contacting the biological material with an effective amount of a compound is disclosed. The compound has the following structure (I): R1—(S)n—R2 ??(I) or a stereoisomer, pharmaceutically acceptable salt or prodrug thereof, wherein R1, R2, and n are as defined herein. Compounds, methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.Type: GrantFiled: October 16, 2009Date of Patent: June 19, 2012Assignee: Ikaria, Inc.Inventors: Edward A. Wintner, Fuqiang Ruan
-
Patent number: 8188291Abstract: The present invention relates to heteroaryl-substituted carboxamides of the formula I, in which Het, A, X, R1, R2 and R3 have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of the formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired.Type: GrantFiled: June 17, 2009Date of Patent: May 29, 2012Assignee: Sanofi-AventisInventors: Hartmut Strobel, Paulus Wohlfart, Heinz-Werner Kleemann, Gerhard Zoller, David William Will
-
Publication number: 20120129812Abstract: Provided is a heterocyclic derivative showing a thyroid hormone ? receptor agonist action, which is effective for the prophylaxis or treatment of the diseases relating to the action. A compound represented by the formula [I]: wherein each symbol is as defined in the specification, a pharmacologically acceptable salt thereof, and a medicament containing the compound as an active ingredient.Type: ApplicationFiled: April 19, 2010Publication date: May 24, 2012Applicant: MITSUBISHI TANABE PHARMA CORPORATIONInventors: Shinji Kawata, Koji Matsumoto, Maki Nijima, Taichi Takahashi
-
Publication number: 20120116088Abstract: In the course of developing 2-[[[2-[(hydroxyacetyl)amino]-4-pyridinyl]methyl]thio]-N-[4-(trifluoromethoxy)phenyl]-3-pyridinecarboxamide (compound A), there are the multiple problems: 1) compound A or its salt is difficult to be recrystallized, the storage stability largely differs depending on the kind of the salt, and it is very difficult to obtain a salt of compound A having excellent storage stability; 2) in a crystallization process of compound A, it is very difficult to control a crystal polymorph, and 3) compound A (free body) causes mineral deposition in the stomach when it is orally administered repeatedly.Type: ApplicationFiled: July 16, 2010Publication date: May 10, 2012Inventors: Masashi Niwa, Hiroshi Deguchi
-
Publication number: 20120101105Abstract: The present invention relates to aryl substituted carboxamide derivatives of formula (I) or a pharmaceutically acceptable salt thereof, which have blocking activities of T-type calcium channels or voltage gated sodium channels as the tetrodotoxin-sensitive (TTX-S) blockers such as Nav1.3 and Nav1.7, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels or voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels or voltage gated sodium channels are involved.Type: ApplicationFiled: May 31, 2010Publication date: April 26, 2012Inventors: Tadashi Inoue, Shuzo Watanabe, Tatsuya Yamagishi, Yoshimasa Arano, Mikio Morita, Kaoru Shimada
-
Publication number: 20120094993Abstract: The present invention relates to compounds of formula I, wherein A, R1 to R7 are defined in the description, and to pharmaceutically acceptable salts thereof. The present invention also relates to the manufacture of such compounds or their pharmaceutically acceptable salts, pharmaceutical compositions containing them and their use as medicaments for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as dyslipidemia, atherosclerosis and cardiovascular diseases.Type: ApplicationFiled: October 7, 2011Publication date: April 19, 2012Inventors: Uwe Grether, Paul Hebeisen, Torsten Hoffmann, Stephan Roever
-
Publication number: 20120095012Abstract: The present invention provides compounds of formula (I), wherein R1 is a monocyclic 5- or 6-membered heteroaryl; R4 is phenyl or monocyclic 5- or 6-membered heteroaryl; and the other substituents as defined in the claims, that inhibit cell and cell division and that inhibit the activation of Hypoxia Inducible Factor (HIF)—mediated transcription and signaling under hypoxic conditions. In one aspect, the compounds of the present invention are useful for the preparation of a medicament for the treatment or prevention of a disease or disorder selected from the group consisting of an inflammatory disease, a hyperproliferative disease or disorder, a hypoxia-related pathology and a disease characterized by excessive vascularisation. Also provided is a pharmaceutical composition, comprising a compound of the invention and a second therapeutic agent or radiation, useful for the treatment or prevention of the mentioned diseases or disorders.Type: ApplicationFiled: December 30, 2009Publication date: April 19, 2012Applicant: Elara Pharmaceuticals GmbHInventors: Jorge Alonson, Arantxa Encinas Lopez, Marcel Muelbaier, Jochen Ammenn, Bernd Wendt, Joe Lewis, Christoph Schultes, Bernd Janssen
-
Publication number: 20120071513Abstract: The present invention provides novel compounds and pharmaceutical compositions thereof, as well as methods for using the compounds and pharmaceutical compositions for treating tumors. Examples of specific tumor types that the compounds may be used to treat include, but are not limited to sarcomas, melanomas, neuroblastomas, carcinomas (including but not limited to lung, renal cell, ovarian, liver, bladder, and pancreatic carcinomas), and mesotheliomas.Type: ApplicationFiled: November 28, 2011Publication date: March 22, 2012Applicant: COMPASS PHARMACEUTICALS LLCInventors: David Kanne, John Ward, Gary Look, X. Michael Wang, Diva Chan, Tina Lee, Donald R. James, Richard Gless, John Schullek, Charles Vacin
-
Patent number: 8124777Abstract: The present invention provides a compound, a photoelectric converter and a photoelectrochemical cell. The complex compound (I) is obtained by coordinating a ligand represented by the formula (II) and a ligand represented by the formula (III) to a metal atom, wherein Y1 and Y2 each independently represent a group including an unsaturated hydrocarbon group and an aromatic ring, R1 and R2 each independently represent a protogenic group or a salt thereof, at least one of R1 and R2 is a protogenic group, R3 and R4 each independently represent an aprotogenic group, R3 and R4 may be bound together, A and B each independently represent a group including an element of group 14, 15, or 16 of the Periodic Table, m and n each independently represent an integer of 0 to 2, a, b, c, and d each independently represent an integer of 0 to 2, and a+b?1.Type: GrantFiled: September 20, 2006Date of Patent: February 28, 2012Assignee: Sumitomo Chemical Company, LimitedInventors: Toshiya Takahashi, Akio Tanaka
-
Patent number: 8124768Abstract: Disclosed are compounds of Formula (I): and salts thereof. Also, disclosed are methods of using the compounds in the treatment of proliferative diseases, such as cancer, and to pharmaceutical compositions comprising at least one compound of Formula (I) or a pharmaceutically acceptable salt.Type: GrantFiled: January 22, 2009Date of Patent: February 28, 2012Assignee: Bristol-Myers Squibb CompanyInventors: Robert M. Borzilleri, Zhen-Wei Cai
-
Patent number: 8106193Abstract: There is described novel organo-platinum luminophores comprising a complex of formula (I). The luminophores have application as the emissive component in organic light emitting diodes.Type: GrantFiled: September 29, 2008Date of Patent: January 31, 2012Assignee: University of YorkInventors: Duncan W. Bruce, Valery Kozhevnikov
-
Publication number: 20120022255Abstract: This invention provides compounds having antiviral activities especially inhibiting activity for influenza virus, more preferably provides substituted 3-hydroxy-4-pyridone derivatives having cap-dependent endonuclease inhibitory activity.Type: ApplicationFiled: March 23, 2010Publication date: January 26, 2012Inventors: Toshio Fujishita, Minako Mikamiyama, Makoto Kawai, Toshiyuki Akiyama
-
Publication number: 20120022261Abstract: The present invention relates to an oxonol dye of formula (I) wherein R1 and R2 are each independently of the other linear or branched C2-C6alkyl residues; R3, R4 and R5 are each independently of the other hydrogen, a C2-C14alkyl residue which may be unsubstituted or hydroxy- or amino-substituted and optionally interrupted by an oxygen atom and R6 is a C2-C14alkyl residue, which may be unsubstituted or hydroxy- or amino-substituted and optionally interrupted by an oxygen atom.Type: ApplicationFiled: September 26, 2011Publication date: January 26, 2012Inventors: Leonhard Feiler, Thomas Raimann
-
Patent number: 8097629Abstract: The invention relates to novel dihydropyridinone derivatives, processes for their preparation, and their use in medicaments, especially for the treatment of chronic obstructive pulmonary diseases, acute coronary syndrome, acute myocardial infarction and heart failure development.Type: GrantFiled: February 5, 2005Date of Patent: January 17, 2012Assignee: Bayer Pharma AktiengesellschaftInventors: Heike Gielen-Haertwig, Barbara Albrecht, Marcus Bauser, Jörg Keldenich, Volkhart Li, Josef Pernerstorfer, Karl-Heinz Schlemmer, Leila Telan
-
Patent number: 8088924Abstract: It was found that the compound having a binding activity to the cannabinoid type 2 receptor represented by the formula (I): wherein R1 is a group represented by the formula: —Y1—Y2—Y3—Ra wherein Y1 is single bond or the like; Y2 is —C(?O)—NH— or the like; Y3 is optionally substituted aryl or the like; R2 is hydrogen or the like; R3 is alkyl or the like; R4 is alkyl or the like; R5 is optionally substituted alkyl or the like; or R3 and R4 taken together with the adjacent atom form cyclic group or the like.Type: GrantFiled: September 2, 2009Date of Patent: January 3, 2012Assignee: Shionogi & Co., Ltd.Inventors: Yukio Tada, Yasuyoshi Iso, Kohji Hanasaki
-
Publication number: 20110319449Abstract: MCHR1 antagonists are provided having the following Formula I: wherein all of the variables are defined herein. Such compounds are useful for the treatment of MCHR1 mediated diseases, such as obesity, diabetes, IBD, depression, and anxiety.Type: ApplicationFiled: March 9, 2010Publication date: December 29, 2011Inventors: Saleem Ahmad, William N. Washburn, Andres S. Hernandez, Jeffrey A. Robl, Khehyong Ngu, Zhenghua Wang
-
Publication number: 20110305729Abstract: Compounds of the invention are of the formula (I); wherein: is a double bond and X is C; or is a single bond and X is N, CH or CQR1; and wherein: n is 1 to 10; R is H or QR1; each R? is independently selected from H and QR1; each Q is independently selected from a bond, CO, NH, S, SO, SO2 or O; each R1 is independently selected from C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, substituted or unsubstituted aryl or heteroaryl, acyl, C1-C10 cycloalkyl, halogen, C1-C10 alkylaryl or C1-C10 heterocycloalkyl; L is a nitrogen-containing heteroaryl; and W is a zinc-chelating residue; or a pharmaceutically acceptable salt thereof. The compounds are useful in therapy.Type: ApplicationFiled: January 26, 2010Publication date: December 15, 2011Inventors: Stephen Joseph Shuttleworth, Cyrille Davy Tomassi
-
Patent number: 8076324Abstract: The present invention relates to di(hetero)arylcyclohexane derivatives of the formula I, in which Ar1, Ar2, R1 and R2 have the meanings indicated in the claims. The compounds of the formula I are valuable pharmaceutical active compounds which inhibit ATP-sensitive potassium channels in the heart muscle and are suitable, for example, for the treatment of disorders of the cardiovascular system such as arrhythmias or a decreased contractility of the heart, such as can occur, for example, in coronary heart disease, cardiac insufficiency or cardiomyopathies. In particular, they are suitable for the prevention of sudden cardiac death. The invention furthermore relates to processes and intermediates for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.Type: GrantFiled: December 3, 2009Date of Patent: December 13, 2011Assignee: Sanofi-AventisInventors: Thomas Bohme, Uwe Gerlach, Dirk Gretzke, Heinz-Werner Kleemann, Stefania Pfeiffer-Marek, Henning Vollert, Jean-Michel Altenburger, Sergio Mallart
-
Publication number: 20110295015Abstract: Disclosed herein is a process for preparing a compound of Formula (I), comprising the steps of: (a) reacting an aniline compound of Formula (II) and an carboxylic acid compound of Formula (III) or an activated carboxylic acid compound thereof, to provide a compound of Formula (IV); and (b) converting said protected amine group attached to said compound of Formula (IV) to an amine group to provide said compound of Formula (I); wherein PAm is a protected amine group. Processes to prepare the compounds of Formulae (II), (III), and (IV) are also disclosed.Type: ApplicationFiled: January 22, 2009Publication date: December 1, 2011Inventors: Robert C Livingston, William P. Gallagher, Robert M. Borzilleri, Zhen-Wei Cai
-
Publication number: 20110294853Abstract: There is provided compounds of formula (I), wherein ring A, D1, D2a, D2b, D3, Y, Y1, L3 and Y3 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of leukotriene C4 synthase is desired and/or required, and particularly in the treatment of a respiratory disorder and/or inflammation.Type: ApplicationFiled: September 10, 2009Publication date: December 1, 2011Inventors: Benjamin Pelcman, Maria Almeida, Martins Katkevics, Peter Nilsson, Wesley Schaal, Kristofer Olofsson
-
Patent number: 8058272Abstract: The present disclosure relates to XIAP inhibitor compound of the formula I:Type: GrantFiled: December 7, 2007Date of Patent: November 15, 2011Assignee: Novartis AGInventors: Zhuoliang Chen, Run-Ming David Wang, Ming Chen, Christopher Sean Straub, Leigh Zawel
-
Publication number: 20110275625Abstract: Disclosed are compounds and compositions of the formula (I) as described herein which are inhibitors of MMP-13. Also disclosed are methods of using and making compounds of the formula (I).Type: ApplicationFiled: November 5, 2009Publication date: November 10, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Neil Alexander Farrow, Donghong Amy Gao, Alexander Heim-Riether, Shuang Liang, Sabine Schlyer, Lana Louise Smith Keenan, Steven John Taylor, Bernd Wellenzohn, Dieter Wiedenmayer, Zhaoming Xiong, Qiang Zhang
-
Patent number: 8053095Abstract: Compounds of formula I may be used in optoelectronic devices wherein R1 is, independently at each occurrence, a C1-C20 aliphatic radical, a C3-C20 aromatic radical, or a C3-C20 cycloaliphatic radical; a is, independently at each occurrence, an integer ranging from 0-4; b is 0, 1 or 2; Ar1 is a direct bond or heteroaryl, aryl, or alkyl or cycloalkyl; Ar2 is heteroaryl, aryl, or alkyl or cycloalkyl; c is an integer ranging from 1-7; and n is an integer ranging from 2-4.Type: GrantFiled: June 5, 2009Date of Patent: November 8, 2011Assignee: General Electric CompanyInventors: Qing Ye, Jie Liu
-
Publication number: 20110263530Abstract: The present invention relates to chemical compounds having a general formula I wherein A1, A2, C1, C2, D, L1, L2, Z and R3, R4, R6, R7 and R8 are defined herein, which are capable of modulating Aurora kinase protein activity, thereby influencing various disease states and conditions related to the activities of Aurora kinase proteins. For example, the compounds are capable of influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, processes of preparing compounds of the invention, synthetic intermediates and methods of treatment of conditions related to the activity of Aurora kinase.Type: ApplicationFiled: June 28, 2011Publication date: October 27, 2011Applicant: Amgen Inc.Inventors: Victor J. CEE, Holly L. Deak, Bingfan Du, Stephanie D. Geuns-Meyer, Brian L. Hodous, Hanh Nho Nguyen, Philip R. Olivieri, Vinod F. Patel, Karina Romero, Laurie Schenkel
-
Patent number: 8039125Abstract: Organic compounds of formula I may be used in optoelectronic devices wherein R1 is, independently at each occurrence, a C1-C20 aliphatic radical, a C3-C20 aromatic radical, or a C3-C20 cycloaliphatic radical; R2 is, independently at each occurrence, a C1-C20 aliphatic radical, a C3-C20 aromatic radical, or a C3-C20 cycloaliphatic radical; a is, independently at each occurrence, an integer ranging from 0-4; b is, independently at each occurrence, an integer ranging from 0-3; Ar1 is a direct bond or heteroaryl, aryl, or alkyl or cycloalkyl; Ar2 is heteroaryl, aryl, or alkyl or cycloalkyl; c is 0, 1 or 2; and n is an integer ranging from 2-4.Type: GrantFiled: October 27, 2008Date of Patent: October 18, 2011Assignee: General Electric CompanyInventors: Qing Ye, Yangang Liang, Shengxia Liu, Kelly Scott Chichak, Jie Liu
-
Publication number: 20110237791Abstract: A 2-pyridone compound represented by the formula [1]: {wherein in the formula [1], the ring represented by A represents a benzene ring or a pyridine ring, X represents any of the structures represented by the formulas [3] shown below: V represents a single bond or a lower alkylene group, and W represents a single bond, an ether bond or a lower alkylene group (wherein the lower alkylene group may contain an ether bond)}, a tautomer or stereoisomer of the compound, a pharmaceutically acceptable salt thereof, or a solvate thereof is a compound that has an excellent GK activating effect and is useful as a pharmaceutical.Type: ApplicationFiled: April 6, 2011Publication date: September 29, 2011Applicants: TAISHO PHARMACEUTICAL CO., LTD, NISSAN CHEMICAL INDUSTRIES, LTD.Inventors: Takanori KAWAGUCHI, Kengo WATATANI, Keiko FUSEGI, Masahiro BOHNO, Hajime ASANUMA, Shoichi KURODA, Yudai IMAI, Tomomichi CHONAN, Nagaaki SATO, Shigeru TOKITA, Shigetada SASAKO, Takumi OKADA, Keishi HAYASHI, Shin ITOH, Noriko SAITO, Rui JIBIKI, Seishi ISHIYAMA, Hirofumi OTA
-
Publication number: 20110230517Abstract: The present invention relates generally to novel calcimimetic compounds and pharmaceutical compositions comprising them. The invention also relates to methods of treating of diseases or disorders related to the function of the calcium sensing receptor using the compounds represented in Formula (I). Where Cy1 is pyridinonyl, pyridinyl, quinolinyl or 9-ethyl-9H-beta-carbolinyl, each of which optionally substituted and where Cy2 is phenyl naphthyl.Type: ApplicationFiled: October 7, 2009Publication date: September 22, 2011Inventors: Christopher Fotsch, Paul Harrington
-
Publication number: 20110212930Abstract: 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: ApplicationFiled: May 5, 2011Publication date: September 1, 2011Applicant: BRISTOL-MYERS SQUIBB COMPANYInventors: 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
-
Publication number: 20110201616Abstract: [Object] A compound which is useful as an EP1 receptor antagonist is provided. [Means for Solution] The present inventors investigated EP1 receptor antagonists, and confirmed that a compound having a sulfonamide structure, in which the nitrogen atom of the sulfonamide structure is substituted with 2-fluoropropyl group, 3-fluoro-2-methylpropyl group or the like, has a potent EP1 receptor antagonistic action, thereby completing the present invention. The sulfonamide compound of the present invention has a potent EP1 receptor antagonistic action and can be used as an agent for preventing and/or treating a lower urinary tract symptom or the like.Type: ApplicationFiled: June 22, 2009Publication date: August 18, 2011Applicant: Astellas Pharma Inc.Inventors: Hideki Kubota, Issei Tsukamoto, Kazunori Kamijo, Koji Kato, Yuta Fukuda, Hidenori Azami
-
Publication number: 20110201603Abstract: The present invention relates to novel Acylaminobenzamide derivatives represented by the following formula (I) and use thereof as pesticides: wherein V represents an aromatic ring group of V1 to V5 described in the detailed description, Q represents an aromatic ring group of Q1 to Q7 described in the detailed description, G1 and G2 represent O or S, R1 represents hydrogen, alkyl, haloalkyl, alkoxy, haloalkoxy, phenyl or a heterocyclic group and R2 and R3 represent hydrogen, alkyl, haloalkyl, alkylcarbonyl, haloalkylcarbonyl, alkoxycarbonyl or haloalkoxycarbonyl.Type: ApplicationFiled: July 30, 2009Publication date: August 18, 2011Applicant: Bayer CropScience AGInventors: Jun Mihara, Tetsuya Murata, Kei Domon, Yukiyoshi Watanabe, Yasushi Yoneta, Takuma Mori, Eiichi Shimojo, Katsuhiko Shibuya, Teruyuki Ichihara, Masashi Ataka, Ulrich Görgens
-
Publication number: 20110200536Abstract: The present invention relates to chelators, in particular to chelators which are capable of forming complexes, i.e. paramagnetic chelates, with paramagnetic metal ions. The invention also relates to said paramagnetic chelates, said paramagnetic chelates linked to other molecules and their use as contrast agents in magnetic resonance imaging (MRI).Type: ApplicationFiled: August 12, 2008Publication date: August 18, 2011Inventors: Harry John Wadsworth, Ian Martin Newington, Dennis O'shea
-
Publication number: 20110195997Abstract: The invention is concerned with dicarboxamide derivatives of formula (I) wherein R1, R2, R3, R4, R5 and R6 are as defined in the specification, as well as physiologically acceptable salts thereof. These compounds inhibit the coagulation factor Xa and can be used in pharmaceutical compositions.Type: ApplicationFiled: April 18, 2011Publication date: August 11, 2011Inventors: Katrin Groebke Zbinden, Wolfgang Haap, Hans Hilpert, Narendra Panday, Fabienne Ricklin
-
Patent number: 7994333Abstract: The present invention relates to the field of anti-inflammatory substances, and more particularly to novel compounds that act as antagonists of the mammalian adhesion proteins known as selectins. In some embodiments, methods for treating selectin mediated disorders are provided which include administration of compound of Formula I: wherein the constituent variables are defined herein.Type: GrantFiled: November 7, 2008Date of Patent: August 9, 2011Assignee: Wyeth LLCInventors: Neelu Kaila, Silvano L. Debarnardo, Kristin M. Janz, Raymond T. Camphausen, Patricia Ward Bedard, Adrian Huang
-
Publication number: 20110183966Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.Type: ApplicationFiled: February 4, 2011Publication date: July 28, 2011Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Francois Maltais, Guy W. Bemis, Tiansheng Wang, Juan Miguel Jimenez, Luca Settimo, Stephen Young, Dean Boyall, Damien Fraysse, Christopher John Davis
-
Publication number: 20110183980Abstract: In one aspect, the invention relates to O-benzyl nicotinamide analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: September 21, 2010Publication date: July 28, 2011Inventors: P. Jeffrey Conn, Craig W. Lindsley, Charles David Weaver, Shaun Stauffer, Richard Williams, Gregor MacDonald, Ya Zhou, José Manuel Bartolomé-Nebreda
-
Publication number: 20110183981Abstract: Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8 and R9, W, X and Y are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals, and inflammatory conditions. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.Type: ApplicationFiled: March 30, 2011Publication date: July 28, 2011Applicant: ARRAY BIOPHARMA INC.Inventors: Allison L. Marlow, Eli Wallace, Jeongbeob Seo, Joseph P. Lyssikatos, Hong Woon Yang, James Blake
-
Publication number: 20110178089Abstract: This invention relates to novel phenyl amide or pyridyl amide derivatives of the formula wherein A1, A2, B1, B2 and R1 to R11 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and can be used as medicaments for the treatment of diseases such as type II diabetes.Type: ApplicationFiled: January 13, 2011Publication date: July 21, 2011Inventors: Caterina Bissantz, Henrietta Dehmlow, Shawn David Erickson, Kyungjin Kim, Rainer E. Martin, Ulrike Obst Sander, Sherrie Lynn Pietranico-Cole, Hans Richter, Christoph Ulmer
-
Publication number: 20110178120Abstract: The present invention relates to pyridoxine (vitamin B6) derived compounds of formula (I), pharmaceutically acceptable salts, or solvates thereof, wherein R1, R2, R4, A, L B1 and B2 are as defined in the specification, and pharmaceutical compositions comprising the compounds. Compounds of formula (I) inhibit Human Immunodeficiency Virus (HIV)-integrase enzyme and are useful for preventing and treating HIV infection and AIDS.Type: ApplicationFiled: June 4, 2009Publication date: July 21, 2011Applicant: AMBRILIA BIOPHARMA, INC.Inventors: Brent Stranix, Francis Beaulieu, Jean-Emmanuel Bouchard, Guy Milot, Wang Zhigang, Réjean Ruel
-
Publication number: 20110178087Abstract: The present invention provides novel compounds and pharmaceutical compositions thereof, as well as methods for using the compounds and pharmaceutical compositions for treating tumors. Examples of specific tumor types that the compounds may be used to treat include, but are not limited to sarcomas, melanomas, neuroblastomas, carcinomas (including but not limited to lung, renal cell, ovarian, liver, bladder, and pancreatic carcinomas), and mesotheliomas.Type: ApplicationFiled: March 30, 2011Publication date: July 21, 2011Applicant: Compass Pharmaceuticals LLC.Inventors: David Kanne, John Ward, Gary Look, X. Michael Wang, Diva Chan, Tina Lee, Donald R. James, Richard Gless, John Schullek, Charles Vacin