Oxadiazoles (including Hydrogenated) Patents (Class 546/269.1)
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Publication number: 20130023525Abstract: The present invention relates to compounds which inhibit bacterial gyrase and/or Topo IV and pharmaceutically acceptable compositions comprising said compounds. These compounds, and compositions thereof, are useful in treating bacterial infection. Accordingly, the present invention also relates to methods for treating bacterial infections in mammals.Type: ApplicationFiled: April 24, 2012Publication date: January 24, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Paul S. Charifson, David D. Deininger, Anne-Laure Grillot, Yusheng Liao, Steven Ronkin, Dean Stamos, Emanuele Perola, Tiansheng Wang, Arnaud Le Tiran, Joseph Drumm
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Publication number: 20130018066Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(?S)—, —S(O)—, —S(O)2—, —C(?O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(?N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(?O)— or —C(?NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(?NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I.Type: ApplicationFiled: July 17, 2012Publication date: January 17, 2013Applicant: Schering Corporation & Pharmacopeia Drug Discovery Inc.Inventors: Zhaoning Zhu, Brian A. McKittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voigt, Corey Strickland, Elizabeth M. Smith, Andrew Stamford, William J. Greenlee, Robert Mazzola, John Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Tao Guo, Thuy X.H. Le, Kurt W. Saionz, Suresh D. Babu, Rachael C. Hunter, Michelle L. Morris, Huizhong Gu, Gang Qian, Dawit Tadesse
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Publication number: 20130018054Abstract: The present invention provides organic compounds of the following structure; A-L1-B—C-D-L2-E that are useful for treating or preventing conditions or disorders associated with DGAT1 activity in animals, particularly humans.Type: ApplicationFiled: September 13, 2012Publication date: January 17, 2013Applicant: NOVARTIS AGInventors: Michael H. SERRANO-WU, Young-shin KWAK, Wenming Liu
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Patent number: 8354436Abstract: The present invention relates to compounds of the general formula (I), and the pharmaceutically acceptable salt or solvate thereof, as anti-inflammatory and immunomodulatory agents.Type: GrantFiled: January 27, 2012Date of Patent: January 15, 2013Assignee: 4SC Discovery GmbHInventors: Johann Leban, Stefan Tasler, Wael Saeb, Carine Chevrier
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Publication number: 20120316147Abstract: The invention relates to a compound of formula (I) wherein R1 to R4 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.Type: ApplicationFiled: June 1, 2012Publication date: December 13, 2012Inventors: Caterina Bissantz, Uwe Grether, Paul Hebeisen, Atsushi Kimbara, Qingping Liu, Matthias Nettekoven, Marco Prunotto, Stephan Roever, Mark Rogers-Evans, Tanja Schulz-Gasch, Christoph Ullmer, Zhiwei Wang, Wulun Yang
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Patent number: 8329725Abstract: The invention relates to annelated pyrrolidin sulfonamides with oxadiazolone headgroup and to their physiologically acceptable salts and physiologically functional derivatives showing PPARdelta or PPARdelta and PPARalpha agonist activity. What is described are compounds of the formula (I), in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparations. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved and demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.Type: GrantFiled: May 22, 2009Date of Patent: December 11, 2012Assignee: SanofiInventors: Stefanie Keil, Matthias Urmann, Wolfgang Wendler, Ulrike Wendler, Maike Glien, Hans Matter, Eugen Falk
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Publication number: 20120302524Abstract: Provided is a 1,3,4-oxadiazole-2-carboxamide compound which has STAT3 inhibitory activity and is useful as an anticancer agent. Provided is a 1,3,4-oxadiazole-2-carboxamide compound represented by formula (I) or a pharmacologically acceptable salt thereof (in the formula, Ar represents a furyl group or the like; R1 represents a hydrogen atom or the like; and —X—Y represents a diaryl group such as a biphenyl group).Type: ApplicationFiled: December 28, 2010Publication date: November 29, 2012Applicants: GENERAL INCORPORATED ASSOCIATION PHARMA VALLEY PROJECT SUPPORTING ORGANIZATION, PHARMA DESIGN, INC., KABUSHIKI KAISHA YAKULT HONSHA, KUMAMOTO HEALTH SCIENCE UNIVERSITY, SHIZUOKA PREFECTUREInventors: Akira Asai, Kenji Matsuno, Naohisa Ogo, Osamu Takahashi, Yoshiaki Masuda, Ayumu Muroya, Yasuto Akiyama, Tadashi Ashizawa, Tadashi Okawara
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Patent number: 8318776Abstract: A pyridine compound represented by the following general formula (1); the pyridine compound in which R1 is a C1-C3 fluoroalkyl group or a C1-C3 fluoroalkoxy group; the pyridine compound in which R2 is a hydrogen atom; the pyridine compound in which R2 is a group represented by Q1; a pesticidal composition containing the pyridine compound as an active ingredient; and a method of controlling a pest including applying an effective amount of the pyridine compound to the pest or a place where the pest inhabits, are provided.Type: GrantFiled: November 18, 2008Date of Patent: November 27, 2012Assignee: Sumitomo Chemical Company, LimitedInventor: Hajime Mizuno
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Publication number: 20120289698Abstract: Provided are compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, X, Z1, Z2, Z3, Z4 and m are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula I, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: April 13, 2012Publication date: November 15, 2012Inventors: Luke W. Ashcraft, Gustave Bergnes, Chihyuan Chuang, Scott Collibee, Pu-Ping Lu, Bradley Morgan, Alex Muci, Xiangping Qian, Jeffrey Warrington, Zhe Yang
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Publication number: 20120283295Abstract: The invention provides an indazole derivative of formula (1), or a pharmaceutically acceptable salt or N-oxide thereof, wherein R1, R2, R3 and R4 are as defined herein. The indazole derivatives are capable of blockading voltage dependent sodium channels and they are useful in the treatment or prevention of normal tension glaucoma, multiple sclerosis, a motorneurone disease, stroke, spinal cord injury, Alzheimer's disease, Parkinson's disease or pain.Type: ApplicationFiled: September 30, 2010Publication date: November 8, 2012Applicant: University College LondonInventors: Cristina Garcia Posada, David Selwood, John Garthwaite, David Baker, Lisa Clutterbuck
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Publication number: 20120264717Abstract: The present invention relates to compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Tables 1-2 or encompassed by formulas I-IV) or compositions thereof, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease.Type: ApplicationFiled: June 18, 2012Publication date: October 18, 2012Inventors: Graham Peter Jones, Kevin James Doyle
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Publication number: 20120258948Abstract: The present invention is directed to a new class of hydroxamic acid derivatives of formula I, wherein the variables G, T, D, L, R1, R2, R3 are as described herein, their use as LpxC inhibitors, and more specifically their use to treat bacterial infections in a patient in need thereof.Type: ApplicationFiled: December 6, 2010Publication date: October 11, 2012Inventors: Matthew Frank Brown, Ye Che, Anthony Marfat, Michael Joseph Melnick, Justin Ian Montgomery, Usa Reilly
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Publication number: 20120258986Abstract: The invention generally relates to the field of nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to new substituted-heterocyclic azole compounds, the synthesis and use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity such as in treating cancer and other neoplastic disorders, inflammatory diseases, disorders of abnormal tissue growth and fibrosis including cardiomyopathy, pulmonary fibrosis, hepatic fibrosis, glomerulonephritis, and other renal disorders, and for the treatment of viral infections (both acute and chronic).Type: ApplicationFiled: January 16, 2012Publication date: October 11, 2012Applicant: KARYOPHARM THERAPEUTICS, INC.Inventors: Vincent P. Sandanayaka, Sharon Shacham, Sharon Shechter, Dilara McCauley
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Publication number: 20120253040Abstract: Disclosed is a compound which is useful as an endothelial lipase inhibitor.Type: ApplicationFiled: December 14, 2010Publication date: October 4, 2012Applicant: Shionogi & Co., Ltd.Inventors: Koji Masuda, Shiro Kida, Naoki Yoshikawa, Manabu Katou, Terukazu Kato, Mado Nakajima, Eiichi Kojima, Mitsuhiro Yonehara
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Patent number: 8278317Abstract: The present invention relates to compounds having the structure (I) useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.Type: GrantFiled: July 18, 2006Date of Patent: October 2, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: B. Wesley Trotter, Kausik K. Nanda, Scott E. Wolkenberg, M. Brad Nolt, David Wisnoski
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Patent number: 8278333Abstract: Object Provided are ?-form crystal, ?-form crystal, and ?-form crystal of a benzoxadiazole derivative, wherein a uniform crystal having sufficient qualities can be obtained with high reproducibility, and they can be anytime supplied as crystals of drug substance for use in producing pharmaceuticals, are particularly suitable for mass synthesis in industrial production, hardly exhibit hygroscopicity and have particularly excellent photo-resistance. Means for Resolution A solving means includes ?-form crystal of 4-[3-isopropyl-5-(6-phenyl-3-pyridyl)-4H-1,2,4-triazol-4-yl]-2,1,3-benzoxadiazole, which shows an endothermic peak at 145 to 150° C. according to a differential scanning calorimeter analysis (DSC analysis) and shows X-ray powder diffraction peaks at 9.8, 11.1, 12.8, 13.3, 17.1, 20.2, 21.2 and 22.3 in 2?(°), and the like.Type: GrantFiled: July 13, 2007Date of Patent: October 2, 2012Assignee: Astellas Pharma Inc.Inventors: Noritaka Hamada, Ryo Mizoguchi, Kuniyuki Sano, Takaaki Sakaida, Yuji Awamura, Yu Iwakawa, Takahiko Tobe, Takashi Sugane
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Publication number: 20120225896Abstract: Disclosed is a novel 2-pyridone derivative represented by general formula (1), which has both angiotensin II receptor antagonist activity and PPAR-? activating activity and is useful as a prophylactic and/or therapeutic agent for cardiovascular diseases and metabolic diseases. Also disclosed is a pharmaceutical composition which contains the novel 2-pyridone derivative. In general formula (1), R1 represents a C1-6 alkyl group or a C1-6 alkoxy group; R2 represents a C1-6 alkyl group or a C3-8 cycloalkyl group; R3 represents a C1-6 alkyl group, a C6-10 aryl-C1-6 alkyl group, a C1-6 alkoxy-C1-6 alkyl group or a group represented by formula (2) (wherein A represents a nitrogen atom or CH, and R5 represents a hydrogen atom or a C1-6 alkoxy group); and R4 represents a group represented by formula (3) or (4).Type: ApplicationFiled: December 22, 2010Publication date: September 6, 2012Applicant: KOWA COMPANY, LTD.Inventors: Toru Miura, Junya Tagashira, Ryohei Sekimoto, Rie Ishida, Hitomi Aoki, Tadaaki Ohgiya
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Publication number: 20120220561Abstract: The present invention relates to compound of formula (I): or pharmaceutically acceptable salts thereof, wherein R1-R5 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: ApplicationFiled: August 12, 2011Publication date: August 30, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Alessandra BARTOLOZZI, Todd BOSANAC, Zhidong CHEN, Stephane DE LOMBAERT, John D. HUBER, Ho Yin LO, Pui Leng LOKE, Weimin LIU, Tina Marie MORWICK, Alan OLAGUE, Doris RIETHER, Heather TYE, Lifen WU, Renee M. ZINDELL
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Publication number: 20120208828Abstract: The present invention relates to new compounds of formula I, to processes for their preparation, to pharmaceutical formulations containing such compounds and to their use in therapy. Such compounds find particular use in the treatment and/or prevention of conditions or diseases which are affected by over-activation of signaling in the Wnt pathway. For example, these may be used in preventing and/or retarding proliferation of tumor cells, for example carcinomas such as colon carcinomas.Type: ApplicationFiled: June 7, 2010Publication date: August 16, 2012Applicant: OSLO UNIVERSITY HOSPITAL HFInventors: Daniel Holsworth, Jo Waaler, Ondrej Machon, Stefan Krauss
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Publication number: 20120184516Abstract: Compounds of Formula I are described. They are useful as stimulators of sGC, particularly NO-independent, heme-dependent stimulators. These compounds may be useful for treating, preventing or managing various disorders that are herein disclosed.Type: ApplicationFiled: June 30, 2011Publication date: July 19, 2012Inventors: Charles Kim, Takashi Nakai, Thomas Wai-Ho Lee, Joel Moore, Nicholas Robert Perl, Jason Rohde, Rajesh R. Iyengar, Ara Mermerian
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Publication number: 20120184544Abstract: The present invention relates to substituted benzamide derivatives of the general Formula I and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, enantiomers, diastereomers, prodrugs, metabolites, and polymorphs and can be useful for treating disease states mediated by glucokinase. Compounds disclosed herein can be used for reducing blood glucose levels and for increasing insulin secretion for treating type II diabetes. The invention also relates to processes for the preparation of the compounds of invention, pharmaceutical compositions containing the compounds, and their use.Type: ApplicationFiled: July 22, 2010Publication date: July 19, 2012Applicant: CADILA HEALTHCARE LIMITEDInventors: Rajendra Kharul, Makul R. Jain, Pankaj R. Patel
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Publication number: 20120184538Abstract: The present invention is concerned with isoxazole-pyridine derivatives of formula I wherein X, R1 to R6 are as described herein. The compounds are active on the GABA A ?5 receptor binding site and useful for the treatment of cognitive disorders, such as Alzheimer's disease.Type: ApplicationFiled: February 10, 2012Publication date: July 19, 2012Inventors: Bernd Buettelmann, Roland Jakob-Roetne, Henner Knust, Matthew C. Lucas, Andrew Thomas
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Publication number: 20120178733Abstract: The present invention is directed to compounds represented by Formula I and pharmaceutically acceptable salts, solvates, hydrates, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to and intermediates used in making such compounds, pharmaceutical compositions containing such compounds, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.Type: ApplicationFiled: August 19, 2011Publication date: July 12, 2012Inventors: Bing-Yan Zhu, Shawn M. Bauer, Zhaozhong J. Jia, Gary D. Probst, Yanchen Zhang, Robert M. Scarborough
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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
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Publication number: 20120165338Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12 and A are as described herein, compositions including the compounds and methods of using the compounds.Type: ApplicationFiled: December 19, 2011Publication date: June 28, 2012Inventors: Johannes Aebi, Alfred Binggeli, Cornelia Hertel, Anish Ashok Konkar, Holger Kuehne, Bernd Kuhn, Hans P. Maerki, Haiyan Wang
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Publication number: 20120157403Abstract: 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: ApplicationFiled: February 24, 2012Publication date: June 21, 2012Inventors: Samuel Chackalamannil, Mariappan V. Chelliah, Yuguang Wang, Yan Xia
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NOVEL SUBSTITUTED PICOLINIC ACIDS, SALTS AND ACID DERIVATIVES THEREOF, AND USE THEREOF AS HERBICIDES
Publication number: 20120157314Abstract: The present invention relates to novel, herbicidally active picolinic acid derivatives of the formula (I) and to processes for preparation thereof. The present invention further provides for the use thereof as a herbicide, especially as a herbicide for selective control of weed plants in useful plant crops, and as a plant growth regulator alone or in combination with safeners and/or in a mixture with other herbicides.Type: ApplicationFiled: October 21, 2011Publication date: June 21, 2012Applicant: BAYER CROPSCIENCE AGInventors: Hartmut AHRENS, Marco BRÜNJES, Hansjörg DIETRICH, Elmar GATZWEILER, Isolde HÄUSER-HAHN, Stefan LEHR, Dirk SCHMUTZLER -
Patent number: 8202856Abstract: The invention relates to compounds of formula I: wherein R1, R2,Ra, Rb, X have the meanings given in claim 16. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis.Type: GrantFiled: December 17, 2008Date of Patent: June 19, 2012Assignee: Merck Serono SAInventors: Anna Quattropani, Christophe Cleva, Eric Sebille, Matthias Schwarz, Delphine Marin, Agnes Bombrun, Wesley Blackaby, Charles Baker-Glenn, Chris Knight, Craig Rouse
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Patent number: 8202865Abstract: The invention relates to compounds of formula I: wherein R1, R2, Ra, Rb, W, Q and S have the meanings given in claim 16. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis.Type: GrantFiled: October 1, 2008Date of Patent: June 19, 2012Assignee: Merck Serono SAInventors: Anna Quattropani, Cyril Montagne, Wolfgang Sauer, Stefano Crosignani, Agnes Bombrun, Mathilde Muzerelle, Jermone Dorbais, Delphine Marin, Jerome Gonzalez, Patrick Gerber
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Publication number: 20120149674Abstract: The instant invention provides compounds of Formula II which are 5-lipoxygenase activating protein inhibitors. Compounds of Formula II are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.Type: ApplicationFiled: February 23, 2012Publication date: June 14, 2012Applicant: Merck Sharpe & Dohme Corp.Inventors: Lin Chu, Bing Li, Anthony K. Ogawa, Hyun O. Ok, Debra L. Ondeyka, Minal Patel, Rosemary Sisco, Feroze Ujjainwalla, Jinyou Xu
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Publication number: 20120142664Abstract: The present invention relates to novel benzyl azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.Type: ApplicationFiled: November 11, 2011Publication date: June 7, 2012Applicant: ALLERGAN, INC.Inventors: Wenkui K. FANG, Liming WANG, Evelyn G. CORPUZ, Ken CHOW, Wha Bin IM
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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
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Publication number: 20120115894Abstract: The present invention is directed to certain Inidazole derivatives which are useful as modulators of Fatty Acid Amide Hydrolase (FAAH) and as FAAH imaging agents. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzeimer Disease, and Parkinson's Disease.Type: ApplicationFiled: February 22, 2010Publication date: May 10, 2012Applicant: Merck Sharp & Dohme Corp.Inventors: Ping Liu, Robert J. DeVita, Linus S. Lin, Marc D. Chioda, Terence G Hamill, Wenping Li
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Patent number: 8163778Abstract: Compounds of formula (I) as well as pharmaceutically acceptable salts and esters thereof wherein the residues have the significance given in claim 1 and which can be used in the form of pharmaceutical compositions.Type: GrantFiled: November 24, 2008Date of Patent: April 24, 2012Assignee: Hoffmann-LA Roche Inc.Inventors: Wolfgang Haap, Paul Hebeisen, Eric Argirios Kitas, Bernd Kuhn, Peter Mohr, Hans Peter Wessel
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Publication number: 20120071460Abstract: The present invention relates to pyrazole oxadiazoles derivatives of Formula (I), and their use for treating multiple sclerosis and other diseases, wherein R1, R2 and R3 are as defined in the description.Type: ApplicationFiled: June 7, 2010Publication date: March 22, 2012Applicant: MERCK SERONO SAInventors: Anna Quattropani, Charles Baker-Glenn, Wesley Blackaby, Chris Knight
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Publication number: 20120064181Abstract: The subject invention relates to novel P2X3 receptor antagonists that play a critical role in treating disease states associated with pain, in particular peripheral pain, inflammatory pain, or tissue injury pain that can be treated using a P2X3 receptor subunit modulator.Type: ApplicationFiled: March 15, 2010Publication date: March 15, 2012Inventors: Christopher S. Burgey, Zhengwu J. Deng, Diem Nguyen, Daniel V. Paone, Craig M. Potteiger, Shaun R. Stauffer, Carolyn Segerdell, Ashley Nomland, John J. Lim
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Publication number: 20120065212Abstract: The present invention relates to compounds of the formula wherein A1, A2, A3 and R1 to R8 are defined in the description, and to pharmaceutically acceptable salts thereof, their manufacture, 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 particularly dyslipidemia, atherosclerosis and cardiovascular diseases.Type: ApplicationFiled: September 7, 2011Publication date: March 15, 2012Inventors: Paul Hebeisen, Hugues Matile, Stephan Roever, Matthew Wright, Sannah Zoffmann Jensen
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Publication number: 20120064121Abstract: The invention relates to compounds that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.Type: ApplicationFiled: July 31, 2008Publication date: March 15, 2012Applicant: SYNTA PHARMACEUTICALS CORP.Inventor: Shoujun Chen
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Patent number: 8134007Abstract: The present invention relates to compounds of the formula (I): and pharmaceutically acceptable salts thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds for the treatment of pain.Type: GrantFiled: May 2, 2008Date of Patent: March 13, 2012Assignee: Pfizer Inc.Inventors: Sharanjeet Kaur Bagal, Karl Richard Gibson, Mark Ian Kemp, Cedric Poinsard, Blanda Luzia Stammen, Stephen Martin Denton, Melanie Susanne Glossop
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Patent number: 8124628Abstract: The instant invention provides compounds of Formula II which are 5-lipoxygenase activating protein inhibitors. Compounds of Formula II are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.Type: GrantFiled: April 6, 2007Date of Patent: February 28, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Lin Chu, Bing Li, Anthony K. Ogawa, Hyun O. Ok, Debra L. Ondeyka, Minal Patel, Rosemary Sisco, Feroze Ujjainwalla, Jinyou Xu
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Publication number: 20120035173Abstract: This invention relates to compounds, pharmaceutical compositions and methods for use in the prevention and treatment of cerebral insufficiency, including enhancement of receptor functioning in synapses in brain networks responsible for basic and higher order behaviors. These brain networks, which are involved in regulation of breathing, and cognitive abilities related to memory impairment, such as is observed in a variety of dementias, in imbalances in neuronal activity between different brain regions, as is suggested in disorders such as Parkinson's disease, schizophrenia, respiratory depression, sleep apneas, attention deficit hyperactivity disorder and affective or mood disorders, among numerous others. In a particular aspect, the invention relates to compounds useful for treatment of such conditions, and methods of using these compounds for such treatment.Type: ApplicationFiled: September 6, 2011Publication date: February 9, 2012Inventors: Leslie Street, Rudolf Mueller, Steven Lee
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Publication number: 20120028953Abstract: Compounds of formula (I) are inhibitors of fatty acid amide hydrolase, (FAAH), and which are useful in the treatment of diseases or medical conditions which benefit from inhibition of FAAH activity, such as anxiety, depression pain, inflammation, and eating, sleep, neurodegenerative and movement disorders: Formula (I) Wherein Ar1 is optionally substituted phenyl or optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms; Ar2 is optionally substituted phenyl, optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms or optionally substituted fused bicyclic heteroaryl having 5 or 6 ring atoms in each fused ring; and Ar3 is a divalent radical selected from the group consisting of optionally substituted phenylene and optionally substituted monocyclic heteroarylene radicals having 5 or 6 ring atoms.Type: ApplicationFiled: February 27, 2009Publication date: February 2, 2012Applicant: VERNALIS (R&D) LTD.Inventors: Stephen Roughley, Steven Walls, Terance Hart, Rachel Parsons, Paul Brough, Christopher Graham, Alba Macias
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Publication number: 20120028931Abstract: Compounds I (R1 is an optionally substituted C1-C13 heteromonocyclic, heterobicyclic or heterotricyclic group containing from 1 to 5 heteroatoms selected from N, O and S; R2 is H, an optionally substituted monocyclic aromatic group, or a C1-C5 heteroaromatic group containing from 1 to 4 heteroatoms selected from N, O and S; R3 is an optionally substituted C1-C13 heteromonocyclic, heterobicyclic or heterotricyclic group containing from 1 to 5 heteroatoms selected from N, O and S; an optionally substituted mono-, bi- or tricyclic C6-C14 aryl group, an optionally substituted C3-C6 cycloalkyl group, or an optionally substituted C3-C6 cycloalkenyl group; each R4, independently for each position capable of substitution, is H or C1-C6 alkyl; R5 is H, halogen or C1-C6 alkyl; m is 0, 1 or 2; n is 0, 1 or 2; p is 0, 1, 2, 3, 4, 5, or 6; and is an optional double bond) and their enantiomers, diastereomers, N-oxides and pharmaceutically acceptable salts, and pharmaceutical compositions containing them, are useful fType: ApplicationFiled: September 14, 2010Publication date: February 2, 2012Applicant: RECORDATI IRELAND LIMITEDInventors: Amedeo Leonardi, Carlo Riva, Luciano Guarneri, Davide Graziani, Fabio Marinoni, Gianni Motta, Ilaria Bettinelli
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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
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Publication number: 20120021007Abstract: The present invention relates to nitric oxide furoxan derivative compounds which showed to be active in the treatment of tumors. In addition, they may be used as adjuvants in cancer immunotherapy.Type: ApplicationFiled: January 15, 2010Publication date: January 26, 2012Inventors: Antonella Viola, Enzo Bronte, Marco Crosetti, Loretta Lazzarato, Roberta Fruttero, Alberto Gasco
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Publication number: 20120022041Abstract: Disclosed are compounds of Formula (I) or pharmaceutically acceptable salts thereof, wherein Q is R1 is cycloalkyl, heteroaryl, or heterocyclyl, each optionally substituted with one to five substituents independently selected from C1 to C6 alkyl, C1 to C4 haloalkyl, —OR4, and/or halogen; and R2, R3, R4, and n are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as vascular disease and autoimmune diseases.Type: ApplicationFiled: January 22, 2010Publication date: January 26, 2012Applicant: BRISTOL-MYERS SQUIBB COMPANYInventors: William J. Pitts, Alaric J. Dyckman, Steven H. Spergel, Scott Hunter Watterson
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Publication number: 20120010212Abstract: The invention relates to a compound of formula wherein A is defined herein or to pharmaceutically active salts, stereoisomeric forms, including individual diastereoisomers and enantiomers of the compound of formula I as well as racemic and non-racemic mixtures thereof. The present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).Type: ApplicationFiled: June 29, 2011Publication date: January 12, 2012Inventors: Matthias Nettekoven, Hasane Ratni, Walter Vifian
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Publication number: 20120004198Abstract: Provided herein are non-peptide GLP-1 receptor modulator compounds, for example, of Formula I, pharmaceutical compositions comprising such compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of a metabolic disorder.Type: ApplicationFiled: February 2, 2011Publication date: January 5, 2012Applicant: ARGUSINA INC.Inventors: Jiayu LIAO, Yufeng Hong, Yong Wang, Thomas W. Von Geldern, Kanyin E. Zhang
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Patent number: 8088802Abstract: An N-phenylarylsulfonylamide compound of formula (I) (R1 is COOH etc.; R2 is hydrogen, methyl, etc.; R3 and R4 are a combination of methyl and methyl, etc.; R5 is isopropyl etc.; Ar is thiazolyl, pyridyl, 5-methyl-2-furyl each optionally substituted with methyl; n is zero or 1), a synthetic intermediate for the compound and a process for its preparation. The compound of formula (I) binds to a prostaglandin E2 receptor, especially an EP1 subtype receptor, and antagonizes it. It is less affected by protein binding, so it has a satisfactory in vivo activity. Therefore, it is considered to be useful as an analgesic, an antipyretic agent, an agent for the treatment of pollakiuria (frequent urination) and/or lower urinary tract disease syndrome or an antineoplastic agent.Type: GrantFiled: October 21, 2009Date of Patent: January 3, 2012Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Atsushi Naganawa, Tetsuji Saito, Kaoru Kobayashi, Takayuki Maruyama, Yoshihiko Nakai, Shinsuke Hashimoto
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Patent number: 8084618Abstract: Heterocyclic compounds derived from benzotriazine, triazines, triazoles and oxadiazoles are disclosed. The methods of synthesis and of use of such heterocyclic compounds are also provided.Type: GrantFiled: January 8, 2010Date of Patent: December 27, 2011Assignee: TargeGen, Inc.Inventors: Wolfgang Wrasidlo, Elena Dneprovskaia