The Additional Hetero Ring Is One Of The Cyclos In A Polycyclo Ring System Patents (Class 514/337)
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Publication number: 20130310378Abstract: The present invention relates to novel 4-(4-pyridyl)-benzamides of the formula (I). The compounds I possess valuable therapeutic properties and are suitable, in particular, for treating diseases that respond to modulation of Rho kinases (ROCKs).Type: ApplicationFiled: April 23, 2013Publication date: November 21, 2013Applicants: AbbVie Inc., AbbVie Deutschland GmbH & Co KGInventors: AbbVie Deutschland GmbH & Co KG, AbbVie Inc.
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Publication number: 20130303544Abstract: The present invention provides a kind of benzopyrone compounds having a structure of formula (I) and the pharmaceutically acceptable salts or prodrugs thereof, and the pharmaceutical compositions containing such compounds, which can be used to regulate the novel estrogen receptor ER-a36, and prevent and/or treat the related diseases mediated by the ER-a36 receptor, such as cancers, etc.Type: ApplicationFiled: December 21, 2011Publication date: November 14, 2013Applicant: BEIJING SHENOGEN PHARMA GROUP LTD.Inventors: Hongxia Ding, Kun Meng, Jin Li
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Publication number: 20130296309Abstract: The present invention provides a compound of formula I; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: July 11, 2013Publication date: November 7, 2013Inventors: Sylvie Chamoin, Qi-Ying Hu, Julien Papillon
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Patent number: 8575351Abstract: Disclosed herein is an active metabolite (“M20”) of a molecule that is useful as a thrombin receptor antagonist: Also disclosed are formulations of this compound, synthetic routes to this compound, and methods of treating a variety of cardiovascular conditions, including acute coronary syndrome and peripheral arterial disease, and of effecting secondary prevention, by orally administering the active metabolilte.Type: GrantFiled: June 2, 2010Date of Patent: November 5, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Kimberly Nguyen Voronin, Natalia A. Penner
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Patent number: 8575198Abstract: The present disclosure provides methods for manufacturing or producing glatiramer acetate having a Mp of 5000-9000 Da.Type: GrantFiled: September 7, 2012Date of Patent: November 5, 2013Assignee: Momenta Pharmaceuticals, Inc.Inventors: Mani S. Iyer, Harper Kaminski
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Publication number: 20130289058Abstract: The invention relates to compounds of formula (I): useful for treating disorders mediated by acyl coA-diacylglycerol acyl transferase 1 (DGAT1), e.g. metabolic disorders. The invention also provides methods of treating such disorders, and compounds and compositions etc. for their treatment.Type: ApplicationFiled: April 26, 2013Publication date: October 31, 2013Inventors: Sejal Patel, Justin Mao, Qian Lui, Rui Zheng, Tyler Harrison, Rohit Duvadie, Xin Chen, Frederic Zecri, Jay Larrow, Xuchun Zheng, Yizong Zhou, Jiong Ye, Yiping Ding, Yu Gai
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Publication number: 20130289074Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2 and m are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.Type: ApplicationFiled: April 24, 2013Publication date: October 31, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Frank HIMMELSBACH, Matthias ECKHARDT, Elke LANGKOPF, Stefan PETERS
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Publication number: 20130289075Abstract: IAP binding molecules and compositions including these are disclosed. The IAP binding molecules interact with IAPB (inhibitor of apoptosis proteins) in cells and may be used to modify apoptosis in cells treated with such molecules. Embodiments of these compounds have a Kd of less than 0.1 micromolar. Methods of using these IAP binding molecules for therapeutic, diagnostic, and assay purposed are also disclosed.Type: ApplicationFiled: June 25, 2013Publication date: October 31, 2013Inventors: Stephen M. Condon, Matthew G. LaPorte, Yijun Deng, Susan R. Rippin
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Publication number: 20130274283Abstract: Premature termination codons readthrough compounds, composition thereof, and methods of making and using the same are provided.Type: ApplicationFiled: February 11, 2013Publication date: October 17, 2013Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Richard A. GATTI, Liutao DU, Robert DAMOISEAUX, Chih-Hung LAI, Michael JUNG, Jin-Mo KU, Carmen BERTONI
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Publication number: 20130273004Abstract: Selected heterocyclic compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like.Type: ApplicationFiled: March 14, 2013Publication date: October 17, 2013Inventors: Guoqing CHEN, Jeffrey A. ADAMS, Jean E. BEMIS, Shon BOOKER, Guolin CAI, Lucian V. DIPIETRO, Celia DOMINGUEZ, Daniel ELBAUM, Julie GERMAIN, Stephanie D. GEUNS-MEYER, Michael K. HANDLEY, Qi HUANG, Joseph L. KIM, Tae-Seong KIM, Alexander S. KISELYOV, Xiaohu OUYANG, Vinod F. PATEL, Leon M. SMITH, II, Markian M. STEC, Andrew TASKER, Ning XI, Shimin XU, Chester YUAN, Michael CROGHAN
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Publication number: 20130267516Abstract: Compounds of general formula I, (formula [I)], their use as calcium receptor-active compounds for the prophylaxis, treatment or amelioration of physiological disorders or diseases associated with disturbances of CaSR activity, such as hyperparathyroidism, pharmaceutical compositions comprising said compounds, and methods of treating diseases with said compounds.Type: ApplicationFiled: November 21, 2011Publication date: October 10, 2013Applicant: LEO PHARMA A/SInventors: Kristoffer Månsson, Lars Kristian Albert Blæhr
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Publication number: 20130267510Abstract: The invention provides compounds of formula (I): Said compounds being inhibitors of Kv3 channels and of use in the prophylaxis or treatment of related disorders.Type: ApplicationFiled: December 6, 2011Publication date: October 10, 2013Applicant: AUTIFONY THERAPEUTICS LIMITEDInventors: Giuseppe Alvaro, Paolo Dambruoso, Simona Tommasi, Anne Decor, Charles Large
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Publication number: 20130261130Abstract: The invention relates to acylamino-phthalic acid amides and related compounds of formula (I) wherein A is —CON—R3R4, —NR5COR6, —NHR7, —OR8, —SR9, —CH2NR10R11, —(CH2)2-R12, —CH?CH—R12, —C?C—R12, optionally substituted phenyl, optionally substituted thiophenyl, or optionally substituted 1,2,3-triazol-4-yl, W is hydrogen, hydroxy or carboxymethoxy, Y is carboxy, methoxycarbonyl or 2H-tetrazol-5-yl, and the various substituents R have the meanings indicated in the description. These compounds are useful for the treatment and/or prophylaxis of skeletal muscle atrophy, schizophrenia and Alzheimer's disease, and as cognitive enhancers.Type: ApplicationFiled: October 31, 2011Publication date: October 3, 2013Inventors: Shaheen Ahmed, Stefan Hettwer, Jan Willem Vrijbloed, Carlo Farina, Hans Allgeier
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Patent number: 8546403Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: GrantFiled: April 12, 2011Date of Patent: October 1, 2013Assignee: Calcimedica, Inc.Inventors: Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
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Publication number: 20130252937Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2 and m are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.Type: ApplicationFiled: March 14, 2013Publication date: September 26, 2013Applicant: Boehringer Ingelheim International GmbHInventors: Matthias ECKHARDT, Sara FRATTINI, Dieter HAMPRECHT, Frank HIMMELSBACH, Elke LANGKOPF, Iain LINGARD, Stefan PETERS, Holger WAGNER
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Publication number: 20130252984Abstract: The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.Type: ApplicationFiled: March 12, 2013Publication date: September 26, 2013Applicant: ALLERGAN, INC.Inventors: Haiqing YUAN, Richard L. BEARD, Xiaoxia LIU, John E. DONELLO, Veena VISWANATH, Michael E. GARST
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Publication number: 20130237552Abstract: The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.Type: ApplicationFiled: April 29, 2013Publication date: September 12, 2013Applicant: ALLERGAN, INC.Inventors: HAIQING YUAN, RICHARD L. BEARD, MICHAEL E. GARST, JOHN E. DONELLO, XIAOXIA LIU, VEENA VISWANATH
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Publication number: 20130231338Abstract: The present invention relates to novel benzofuran-2-sulfonamide derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.Type: ApplicationFiled: March 1, 2013Publication date: September 5, 2013Applicant: ALLERGAN, INC.Inventors: HAIQING YUAN, RICHARD L. BEARD, XIAOXIA LIU, JOHN E. DONELLO, VEENA VISWANATH, MICHAEL E. GARST
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Publication number: 20130231371Abstract: A spot-on pesticide composition for animals, specifically mammals, namely dogs, which composition comprises a combination of a pyrethroid and a macrocyclic lactone selected from avermectin, ivermectin, selamectin, moxidectin, milbemycin and any combination thereof, and optionally fipronil and/or an insect growth regulator, in doses and proportions which are parasiticidally effective against a variety of insects and pests, and in a formulation which is convenient for local application to the animal's skin, preferably localized over a small surface area.Type: ApplicationFiled: April 5, 2013Publication date: September 5, 2013Applicant: Sergeant's Pet Care Products, Inc.Inventors: Larry Nouvel, Donald W Kelley
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Publication number: 20130231325Abstract: Disclosed are novel isoflavone derivatives having the structure of Formula I: which are ALDH-2 inhibitors, useful for treating a patient in need thereof, for dependence upon drugs of addiction, for example addiction to dopamine-producing agent such as cocaine, morphine, amphetamines, nicotine, and alcohol.Type: ApplicationFiled: August 30, 2012Publication date: September 5, 2013Applicant: Gilead Sciences. Inc.Inventors: Michael Graupe, Chandrasekar Venkataramani, Jeff Zablocki
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Publication number: 20130231339Abstract: The present invention relates to novel benzofuran-2-sulfonamide pyridine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.Type: ApplicationFiled: March 1, 2013Publication date: September 5, 2013Applicant: ALLERGAN, INC.Inventors: HAIQING YUAN, RICHARD L. BEARD, XIAOXIA LIU, JOHN E. DONELLO, VEENA VISWANATH, MICHAEL E. GARST
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Patent number: 8519142Abstract: The present invention provides a compound of formula I; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: GrantFiled: September 14, 2012Date of Patent: August 27, 2013Assignee: Novartis AGInventors: Sylvie Chamoin, Qi-Ying Hu, Julien Papillon
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Publication number: 20130217726Abstract: The present invention relates to inhibitors of insulin-regulated aminopeptidase (IRAP) and methods for inhibiting same, as well as compositions comprising said inhibitors. In particular, the inhibitors of the present invention may be useful in therapeutic applications including enhancing memory and learning functions.Type: ApplicationFiled: February 6, 2013Publication date: August 22, 2013Applicants: ST. VINCENT'S INSTITUTE OF MEDICAL RESEARCH, HOWARD FLOREY INSTITUTEInventors: Howard Florey Institute, St. Vincent's Institute of Medical Research
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Publication number: 20130217730Abstract: The present invention refers to compounds of formula (I): as well as to a method for their preparation, pharmaceutical compositions comprising the same, and use thereof for the treatment and/or chemoprevention of cancer, aging related diseases or processes, diabetes and neurodegenerative diseases.Type: ApplicationFiled: May 10, 2011Publication date: August 22, 2013Applicant: IKERCHEM, S.L.Inventors: Fernando Pedro Cossio Mora, Leire Lidia Arias Echeverría, Yosu Ion Vara Zalazar, Eneko Aldaba Arévalo, Eider San Sebastián Larzabal, Aizpea Zubia Olascoaga
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Publication number: 20130217704Abstract: Methods of inhibiting cytochrome P450 2D6 enzymes are provided that can be used for improving the treatment of diseases by preventing degradation of drugs or other molecules by cytochrome P450 2D6. Pharmaceutical compositions are provided that can act as boosters to improve the pharmacokinetics, enhance the bioavailability, and enhance the therapeutic effect of drugs that undergo in vivo degradation by cytochrome P450 2D6 enzymes.Type: ApplicationFiled: April 1, 2013Publication date: August 22, 2013Inventor: Sequoia Pharmaceuticals, Inc.
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Patent number: 8513280Abstract: The present invention is about the use of at least one epothilone or derivative thereof as an active ingredient for manufacturing a medicament for use in the treatment of disease(s) involving a neuronal connectivity defect.Type: GrantFiled: September 9, 2010Date of Patent: August 20, 2013Assignees: Institut National de la Sante et de la Recherche Medicale, Commissariat a l'Energie Atomique, Gesellschaft fur Biotechnologische Forschung mbH (GBF)Inventors: Annie Andrieux, Didier Job, Annie Schweitzer, Gerhard Höfle
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Publication number: 20130212715Abstract: It has been discovered that STAT5 phosphorylation and CD150 are effective biomarkers for detecting, diagnosing, and monitoring hematological malignancies, including for example lymphomas. Compositions and methods for identifying therapeutic agents for the treatment of hematologic malignancies using p-STAT5, CD150 or both as biomarkers are described.Type: ApplicationFiled: February 7, 2013Publication date: August 15, 2013Applicant: Georgia Health Sciences University Research Institute, Inc.Inventor: Georgia Health Sciences University Research Institute, Inc.
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Publication number: 20130210858Abstract: The present invention relates to sulfamoyl benzoic acid heterobicyclic derivatives of the formula (I) or a pharmaceutically acceptable salt thereof or a prodrug thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders which are mediated via the TRPM8 receptor.Type: ApplicationFiled: October 3, 2011Publication date: August 15, 2013Applicant: Raqualia Pharma Inc.Inventors: Kiyoshi Kawamura, Yuji Shishido, Masashi Ohmi
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Publication number: 20130210772Abstract: Described herein are pharmaceutical compositions and medicaments, and methods of using such pharmaceutical compositions and medicaments in the treatment of cancer.Type: ApplicationFiled: April 15, 2011Publication date: August 15, 2013Applicant: COLBY PHARMACEUTICAL COMPANYInventors: Hirak S. Basu, David A. Zarling, George Wilding, Farideh Mehraein-Ghomi, Dawn R. Church
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Patent number: 8507687Abstract: The present invention relates to a substantially a solid form of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid (Compound 1, Solvate Form A and Compound 1, HCl Salt Form A), processes for making such forms, pharmaceutical compositions thereof, and methods of treatment therewith.Type: GrantFiled: April 7, 2011Date of Patent: August 13, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Ali Keshavarz-Shokri, Beili Zhang, Mariusz Krawiec
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Publication number: 20130203739Abstract: [Problem] To provide a GPR40 activating agent having, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the salt or the compound, or the like, particularly, an insulin secretagogues and a prophylactic and/or therapeutic agent against diabetes, obesity, or other diseases. [Means of solving the problem] A compound of Formula (1): (where n is 0 to 2; p is 0 to 4; h is 0 to 3; j is 0 to 3; k is 0 to 2; a ring B is an aryl group or a heteroaryl group; X is O, S, or —NR7—; J1 is —CR11aR11b— or —NR11c—; J2 is —CR12aR12b— or —NR12c—; and R1 to R12c are specific groups), a salt of the compound, or a solvate of the salt or the compound.Type: ApplicationFiled: October 11, 2011Publication date: August 8, 2013Applicant: MOCHIDA PHARMACEUTICAL CO., LTD.Inventors: Akihiro Okano, Munetaka Ohkouchi, Muneyoshi Makabe
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Publication number: 20130203747Abstract: Compounds of formula I: wherein a, R1, R2, R3, R4, R5 and R6 are defined herein, are useful as inhibitors of HIV replication.Type: ApplicationFiled: November 21, 2012Publication date: August 8, 2013Applicant: Gilead Sciences, Inc.Inventor: Gilead Sciences, Inc.
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Publication number: 20130202667Abstract: The present invention relates to hydrogel particles coated with lipid, which are made from dispersing hydrogel particles in an organic solvent in which lipids are dissolved, and to a method for manufacturing same. Unlike the existing method for manufacturing hydrogel core vesicles, the present invention can effectively manufacture same by using an emulsification method, without involving the steps of chemical treatment of the surface of hydrogels or dilution, thereby facilitating mass production and preventing the decrease of drug encapsulation efficiency.Type: ApplicationFiled: October 12, 2011Publication date: August 8, 2013Applicant: AMOREPACIFIC CORPORATIONInventors: Eun Jung An, Do Hoon Kim, Hyung Jun Lim, Jong Won Shim, Choon Bok Jeong, Lee Kyoung Kwon, Jun Oh Kim
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Publication number: 20130196987Abstract: The present invention provides compounds, methods for the synthesis thereof and methods for the use thereof in the treatment of various disorders including inflammatory or autoimmune disorders, and disorders involving malignancy or increased angiogenesis.Type: ApplicationFiled: October 30, 2012Publication date: August 1, 2013Applicant: EISAI CO., LTD.Inventors: Roch Boivin, Kenichi Chiba, Jesse Chow, Hong Du, Yoshihito Eguchi, Masanori Fujita, Masaki Goto, Fabian Gusovsky, Jean-Christophe Harmange, Atsushi Inoue, Yimin Jiang, Megumi Kawada, Takatoshi Kawai, Yoshiyuki Kawakami, Akifumi Kimura, Makoto Kotake, Yoshikazu Kuboi, Charles-Andre Lemelin, Xiang-Yi Li, Tomohiro Matsushima, Yoshiharu Mizui, Kenzo Muramoto, Hideki Sakurai, Yong-Chun Shen, Hiroshi Shirota, Mark Spyvee, Isao Tanaka, John (Yuan) Wang, Satoshi Yamamoto, Naoki Yoneda
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Publication number: 20130197013Abstract: The invention relates to cyclopropylamine compounds, in particular the compounds of Formula (I), and their use in therapy, including e.g. in the treatment or prevention of cancer, a neurological disease or condition, or viral infection.Type: ApplicationFiled: July 27, 2011Publication date: August 1, 2013Inventors: Mathew Colin Thor Fyfe, Alberto Ortega Muñoz, Julio Castro-Palomino Laria, Marc Martinell Pedemonte, Maria de los Ángeles Estiarte-Martínez, Nuria Valls Vidal
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Publication number: 20130190338Abstract: The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.Type: ApplicationFiled: March 11, 2013Publication date: July 25, 2013Applicant: ALLERGAN, INC.Inventor: ALLERGAN, INC.
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Publication number: 20130172390Abstract: The present invention relates to halogen-substituted amide derivatives of the general formula (I) in which R1 to R6, Q1 to Q8, A, V, W, X, Y, n and m are each defined as described in the description—and to a process for preparation thereof and to the use thereof as insecticides and acaricides.Type: ApplicationFiled: September 14, 2012Publication date: July 4, 2013Applicant: Bayer Intellectual Property GmbHInventors: Markus Heil, Eike Kevin Heilmann, Alexander Sudau, Tobias Kapferer, Friedrich August Mühlthau, Peter Jeschke, Arnd Voerste, Ulrich Görgens, Klaus Raming, Ulrich Ebbinghaus-Kintscher, Mark Drewes, Martin Adamczewski, Angela Becker
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Publication number: 20130172339Abstract: A compound of formula (I), wherein A is S, O or a double bond, and L is a substituted thiazolyl, phenyl or pyridyl. The compound is useful for the treatment of inflammation and cancer.Type: ApplicationFiled: September 19, 2011Publication date: July 4, 2013Applicant: KANCERA ABInventors: Styrbjorn Bystrom, Charles Hedgecock, Evert Homan, Thomas Lundback, Jessica Martinsson, Meral Sari, Katarina Farnegardh, Mattias Jonsson
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Patent number: 8476313Abstract: Compounds and methods useful for treating and prevention of cancer, particularly hormone-dependent breast cancer. Provided are compounds of formula I: wherein X is selected from O, N, S, SO, SO2, and S(CH2)n, wherein n=1-10; R1 and R2 may be the same or different and are selected from H, OH, OCH3, OCH2CH3, OCH2C6H5, NH2, NHCH3, N(CH3)2, CH3, CH2CH3, CH2CH2CH3, CH(CH3)2, C(CH3)3, NO2, F, Cl, Br, CF3, SH, SCH3, SCH2CH3, OCOCH3, OCOC(CH3)3, OCOCH2COOH, and CN; and R3 is a nitrogen-containing heterocyclic ring. Also provided are method for treating or preventing cancer in a subject by administering a therapeutically effective amount of a heteroaryl-containing isoflavone, or a pharmaceutically acceptable salt or prodrug thereof, to a subject in need of treatment.Type: GrantFiled: May 26, 2009Date of Patent: July 2, 2013Assignee: The Ohio State University Research FoundationInventors: Robert W. Brueggemeier, Young-Woo Kim, John C. Hackett
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Publication number: 20130165460Abstract: The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.Type: ApplicationFiled: February 20, 2013Publication date: June 27, 2013Applicant: ALLERGAN, INC.Inventor: ALLERGAN, INC.
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Publication number: 20130164218Abstract: This disclosure relates to Hypoxia Inducible Factor-1 pathway inhibitors and uses as anticancer and imaging agents. In certain embodiments, the disclosure contemplates compounds and pharmaceutical compositions disclosed herein.Type: ApplicationFiled: December 27, 2012Publication date: June 27, 2013Applicant: EMORY UNIVERSITYInventor: EMORY UNIVERSITY
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Patent number: 8466175Abstract: The present invention relates to a novel form of the (?)-enantiomer of 5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)-methyl]sulfinyl]-1H-benzimidazole, i.e. S-omeprazole. More specifically, it relates to a novel form of the magnesium salt of the S-enantiomer of omeprazole trihydrate. The present invention also relates to processes for preparing such a form of the magnesium salt of S-omeprazole and pharmaceutical compositions containing it. Furthermore, the present invention also relates to new intermediates used in the process.Type: GrantFiled: November 17, 2011Date of Patent: June 18, 2013Assignee: AstraZeneca ABInventors: Hanna Cotton, Anders Kronström, Anders Mattson, Eva Möller
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Patent number: 8466166Abstract: This invention relates to compounds of the formula (I): or a pharmaceutically acceptable salt thereof, wherein: R1, R2, R3, R4, A and E are each as described herein or a pharmaceutically acceptable salt, and compositions containing such compounds and the method of treatment and the use, comprising such compounds for the treatment of a condition mediated by acid pump antagonistic activity such as, but not limited to, as gastrointestinal disease, gastroesophageal disease, gastroesophageal reflux disease (GERD), laryngopharyngeal reflux disease, peptic ulcer, gastric ulcer, duodenal ulcer, NSAID-induced ulcers, gastritis, infection of Helicobacter pylori, dyspepsia, functional dyspepsia, Zolli?ger-Ellison syndrome, non-erosive reflux disease (NERD), visceral pain, cancer, heartburn, nausea, esophagitis, dysphagia, hypersalivation, airway disorders or asthma.Type: GrantFiled: September 17, 2007Date of Patent: June 18, 2013Assignee: Raqualia Pharma Inc.Inventors: Hiroki Koike, Mikio Morita
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Patent number: 8461300Abstract: Sequence-specific polymers are proving to be a powerful approach to assembly and manipulation of matter on the nanometer scale. Ligands that are peptoids, or sequence-specific N-functional glycine oligomers, allow precise and flexible control over the arrangement of binding groups, steric spacers, charge, and other functionality. We have synthesized short peptoids that can prevent the aggregation of gold nanoparticles in high-salt environments including divalent salt, and allow co-adsorption of a single DNA molecule. This degree of precision and versatility is likely to prove essential in bottom-up assembly of nanostructures and in biomedical applications of nanomaterials.Type: GrantFiled: January 12, 2011Date of Patent: June 11, 2013Assignee: Sandia CorporationInventors: David Bruce Robinson, Ronald Zuckermann, George M. Buffleben
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Publication number: 20130137648Abstract: Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme.Type: ApplicationFiled: January 23, 2013Publication date: May 30, 2013Applicant: Chiesi Farmaceutici S.p.A.Inventor: Chiesi Farmaceutici S.p.A.
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Publication number: 20130131036Abstract: Disclosed herein are modulators of TRPV3 of formula (II): wherein G1, X1, X2, X3, X4, X5, G2, Ra, Rb, and u are as defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also presented.Type: ApplicationFiled: October 23, 2012Publication date: May 23, 2013Applicant: AbbVie Inc.Inventor: AbbVie Inc.
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Publication number: 20130123305Abstract: The present invention relates to hydroximoyl-tetrazole derivatives of formula (I), their process of preparation, their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions. wherein A represents a tetrazoyl group, Het represents a pyridyl group or a thiazolyl group and X represents various substituents.Type: ApplicationFiled: December 28, 2010Publication date: May 16, 2013Inventors: Christian Beier, Jurgen Benting, David Bernier, Pierre-Yves Coqueron, Philippe Desbordes, Christophe Dubost, Stephanie Gary, Pierre Genix, Daniela Portz, Ulrike Wachendorff-Neumann
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Publication number: 20130123265Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases, disorders or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: January 4, 2013Publication date: May 16, 2013Applicant: CalciMedica, Inc.Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Frank King, Yazhong Pei, Jeffrey P. Whitten
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Publication number: 20130116247Abstract: Compounds which directly inhibit IRE-1? activity in vitro, prodrugs, and pharmaceutically acceptable salts there-of. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response or with regulated IRE1-dependent decay (RIDD) and can be used as single agents or in combination therapies.Type: ApplicationFiled: April 5, 2011Publication date: May 9, 2013Applicant: MANNKIND CORPORATIONInventors: Qingping Zeng, Andras Toro, John Bruce Patterson, Warren Stanfield Wade, Zoltan Zubovics, Yun Yang, Zhipeng Wu
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Publication number: 20130109671Abstract: Provided herein are methods of treating or ameliorating a pediatric cholestatic liver disease by non-systemically administering to an individual in need thereof a therapeutically effective amount of a pediatric formulation comprising an Apical Sodium-dependent Bile Acid Transporter Inhibitor (ASBTI) or a pharmaceutically acceptable salt thereof. Also provided are methods for treating or ameliorating a pediatric liver disease, decreasing the levels of serum bile acids or hepatic bile acids, treating or ameliorating pruritis, reducing liver enzymes, or reducing bilirubin comprising non-systemically administering to an individual in need thereof a therapeutically effective amount of a pediatric formulation comprising an ASBTI or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: October 26, 2012Publication date: May 2, 2013Applicant: Lumena Pharmaceuticals, Inc.Inventor: Lumena Pharmaceuticals, Inc.