Spiro Ring System Patents (Class 514/278)
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Publication number: 20150065517Abstract: 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: November 10, 2014Publication date: March 5, 2015Applicant: NOVARTIS AGInventors: Michael H. SERRANO-WU, Young-shin KWAK, Wenming LIU
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Publication number: 20150065471Abstract: The present invention is directed to a pharmaceutically acceptable crystalline addition salt of 5-[(1R)-2-({2-[4-({4-(2,2-difluoro-2-phenylethoxy)phenyl]ethyl}amino)-1-hydroxyethyl]-8-hydroxyquinolin-2(1H)-one, and (ii) a dicarboxylic acid, a sulfonic acid or a sulfimide, or a pharmaceutically acceptable solvate thereof.Type: ApplicationFiled: March 28, 2013Publication date: March 5, 2015Inventors: Carlos Puig Duran, Francesc Carrera Carrera, Juan Bautista Pérez Garcia, Enrique Moyes Valles, Iolanda Marchueta Hereu
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Patent number: 8969325Abstract: Disclosed herein are compounds of formula (I): or pharmaceutically acceptable salts thereof, wherein X1, L, Rx, Ry, G, Z, A, m, n, and p are as defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.Type: GrantFiled: December 17, 2012Date of Patent: March 3, 2015Assignee: AbbVie Inc.Inventors: Michael J. Dart, Philip R. Kym, Eric A. Voight, Anurupa Shrestha, Jerome F. Daanen, Tammie K. Jinkerson, Ryan G. Keddy, Sridhar Peddi, Arthur Gomtsyan, Michael E. Kort, Gregory A. Gfesser, Kevin R. Woller, Derek W. Nelson
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Patent number: 8969564Abstract: The present disclosure is generally directed to compounds which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds, and methods for inhibiting AAK1.Type: GrantFiled: February 24, 2014Date of Patent: March 3, 2015Assignee: Bristol-Myers Squibb CompanyInventors: Vivekananda M. Vrudhula, Senliang Pan, Ramkumar Rajamani, John E. Macor, Joanne J. Bronson, Carolyn Diane Dzierba, Susheel Jethanand Nara, Maheswaran Sivasamban Karatholuvhu
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Publication number: 20150057302Abstract: This invention relates to spiroindoline compounds for the treatment of helminth infections and the treatment of parasitosis, such as caused by helminth infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. Moreover this invention relates to pharmaceutical compositions and kits comprising the compounds.Type: ApplicationFiled: October 14, 2014Publication date: February 26, 2015Inventors: Jürgen LUTZ, Sandra KOCH, Manfred UPHOFF, Anja Regina HECKEROTH, Britta von OEPEN, Ulrich SONDERN, Christophe Pierre Alain CHASSAING
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Publication number: 20150057268Abstract: Neuropeptide S receptor antagonists are provided that bind in functional assays to neuropeptide S receptors; methods are provided for use of these antagonists in treatment of conditions or disease states that are ameliorated by blocking of the neuropeptide S receptor, including substance abuse and substance abuse relapse; and for use of neuropeptide S receptor antagonists in the manufacture of therapeutics and pro-drugs for therapeutics useful in disease states and conditions sensitive to binding of the neuropeptide S receptor.Type: ApplicationFiled: December 6, 2012Publication date: February 26, 2015Applicant: RESEARCH TRIANGLE INSTITUTEInventors: Scott Runyon, Yanan Zhang, Carla Hassler, Brian Gilmour
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Publication number: 20150057279Abstract: This invention relates to certain heteroaryl compounds which may be used as medicaments, more specifically as medicaments for treating animals. The medicament can be used for the treatment of parasitic infections such as helminth infections and the treatment of parasitosis caused by such infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. This invention also relates to pharmaceutical compositions and kits comprising the compounds.Type: ApplicationFiled: March 27, 2013Publication date: February 26, 2015Inventors: Michael Berger, Marko Eck, Christopher Kern
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Patent number: 8962608Abstract: The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.Type: GrantFiled: September 21, 2012Date of Patent: February 24, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Jason Brubaker, Christopher Dinsmore, Dawn Marie Hoffman, Joon Jung, Duan Liu, Scott Peterson, Tony Siu, Luis E. Torres, Hongjun Zhang, Zhongyong Wei, Feng Shi
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Publication number: 20150051239Abstract: This invention concerns arylsulfonyl pyrazoline carboxamidine derivatives as antagonists of 5-ht6 receptors, to methods for the preparation of these compounds and to novel intermediates useful for their synthesis.Type: ApplicationFiled: October 29, 2014Publication date: February 19, 2015Inventors: Arnold van Loevezijn, Wouter I. Iwema Bakker, Alex Stoit, Agatha M. Rensink, Jennifer Venhorst, Martina A.W. Van Der Neut, Martin De Haan, Cornelis G. Kruse
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Patent number: 8957070Abstract: The present invention provides a glucokinase activator containing a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof or a prodrug thereof. According to the present invention, a glucokinase activator useful as a pharmaceutical agent such as agent for the prophylaxis or treatment of diabetes, obesity and the like, and the like can be provided.Type: GrantFiled: April 20, 2006Date of Patent: February 17, 2015Assignee: Takeda Pharmaceutical Company LimitedInventors: Tsuneo Yasuma, Osamu Ujikawa
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Patent number: 8957083Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A1, A3, A4, A5, A6, A8, L, R2, R7, R9, W and Y of Formula I are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to plaque formation and deposition, resulting from the activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formulas II and III, sub-Formula embodiments of Formulas I, II and III, intermediates and processes and methods useful for the preparation of compounds of Formulae I-III.Type: GrantFiled: November 18, 2011Date of Patent: February 17, 2015Assignee: Amgen Inc.Inventors: Ana Elena Minatti, Oleg Epstein, Ryan White, Matthew Weiss, Wenge Zhong, Jonathan D. Low
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Publication number: 20150045347Abstract: Compounds having the following formula: (I) wherein: A is an optionally substituted triazole, or a stereoisomer or a pharmaceutically-acceptable salt thereof, are useful as kinase modulators, including IRAK-4 modulation.Type: ApplicationFiled: January 11, 2013Publication date: February 12, 2015Inventors: Dharmpal S. Dodd, Christopher P. Mussari, Rajeev S. Bhide, Satheesh Kesavan Nair, Venkatram Reddy Paidi, Sreekantha Ratna Kumar, Abhisek Banerjee, Ramesh Sistla, William J. Pitts, John Hynes
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Publication number: 20150044283Abstract: Single oral solid dosage form comprising an immediate release first dosage composition having at least two antibiotic agents and a delayed release second dosage composition having a proton pump inhibitor are provided herein. The single oral solid dosage form according to some aspects of the invention can be used for the treatment of disorders associated with infection by H. pylori or the prevention of recurrence of disorders associated with infection by H. pylori.Type: ApplicationFiled: October 24, 2014Publication date: February 12, 2015Inventors: Reza Fathi, Gilead Raday, Guy Goldberg, Patrick Gosselin
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Publication number: 20150045363Abstract: Hedgehog pathway inhibitors, such as small molecules, are used to prevent, slow, block the formation of cartilage tumors as well as exostosis or enchondromas.Type: ApplicationFiled: March 14, 2013Publication date: February 12, 2015Inventors: Wentian Yang, Benjamin G. Neel
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Patent number: 8952166Abstract: The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and conditions associated with excessive salt and water retention.Type: GrantFiled: July 25, 2013Date of Patent: February 10, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Fa-Xiang Ding, Shuzhi Dong, Jessica Frie, Xin Gu, Jinlong Jiang, Alexander Pasternak, Haifeng Tang, Zhicai Wu, Yang Yu, Takao Suzuki
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Patent number: 8952158Abstract: The present invention relates to the compound represented by formula (I): (wherein, all the symbols have the same meaning as that of the specification), a salt thereof, a solvate thereof or a prodrug thereof. Since the compound of the present invention has an anti stress action, it is useful for preventive and/or therapeutic agent for a disease caused by stress, especially a digestive system disease caused by stress and is superior to oral absorption.Type: GrantFiled: May 17, 2013Date of Patent: February 10, 2015Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Kazuyuki Ohmoto, Masashi Kato, Yoshifumi Kagamiishi, Junichiro Manako
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Publication number: 20150038490Abstract: The present invention is directed to spiropyrrolidine compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.Type: ApplicationFiled: October 20, 2014Publication date: February 5, 2015Applicant: Merck Sharp & Dohme Corp.Inventors: Kun Liu, Shawn J. Stachel, Craig A. Coburn, Thomas G. Steele, Richard Soll, Hao Wu, Xuanjin Peng, Yaxian Cai, Xiaoxiang Du, Jian Li
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Patent number: 8945632Abstract: The current invention provides therapeutic methods which include inhibition of nuclear factor ?b pathway in a cell based on the discovery of an active fraction of a plant extract termed NUP or a composition which includes NUP. NUP is used in treating and managing different diseases such as cancer, inflammation, and virus infections.Type: GrantFiled: July 19, 2011Date of Patent: February 3, 2015Assignees: Ben Gurion University of the Negev R&D Authority, Mor Research Applications Ltd.Inventors: Avi Golan, Jacob Gopas, Janet Ozer, Nadav Eisner, Adelbert Bacher, Wolfgang Eisenreich, Elena Ostrozhenkova, Hila Winer
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Patent number: 8945627Abstract: The invention provides biocompatible micelles loaded with one or more active agents. The micelles can encapsulate anticancer drugs such as gossypol, and combinations of drugs, such as gossypol and paclitaxel, gossypol and 17-AAG, gossypol and cyclopamine, gossypol, paclitaxel, and 17-AAG, and gossypol, paclitaxel, and cyclopamine. The micelle compositions provide effective solubilization of difficult to solubilize drug combinations without the need for additional surfactants that can be toxic to patients. Thus, the invention provides stable and biocompatible drug formulations that improve bioavailability without causing toxicity.Type: GrantFiled: May 4, 2012Date of Patent: February 3, 2015Assignee: Wisconsin Alumni Research FoundationInventors: Glen S. Kwon, Ho-Chul Shin, Hyunah Cho
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Publication number: 20150031691Abstract: The present invention relates to compounds represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. Definitions for the variables are provided herein.Type: ApplicationFiled: October 8, 2014Publication date: January 29, 2015Inventors: Lawrence Wayne Dillard, Jing Yuan, Katerina Leftheris, Shankar Venkatraman, Guosheng Wu, Lanqi Jia, Zhenrong Xu, Salvacion Cacatian, Angel Morales-Ramos, Suresh B. Singh, Yajun Zheng
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Publication number: 20150031673Abstract: Compounds of formula (I): wherein A1, A2, Ra, Rb, Rc, Rd, R3, R4, R5 and T are as defined in the description. Medicinal products containing the same which are useful in treating pathologies involving a deficit in apoptosis, such as cancer, auto-immune diseases, and diseases of the immune system.Type: ApplicationFiled: July 21, 2014Publication date: January 29, 2015Inventors: Arnaud LE TIRAN, Thierry LE DIGUARHER, Jérôme-Benoît STARCK, Jean-Michel HENLIN, Anne-Françoise GUILLOUZIC, Guillaume DE NANTEUIL, Olivier GENESTE, Imre FEJES, Janos TATAI, Miklos NYERGES, James Edward Paul DAVIDSON, James Brooke MURRAY, I-Jen CHEN, Didier DURAND
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Publication number: 20150031541Abstract: Compounds of the formula (I) wherein the substituents are as defined in claim 1, are useful as a pesticides.Type: ApplicationFiled: February 27, 2013Publication date: January 29, 2015Applicant: Syngenta Participations AGInventors: Clemens Lamberth, Sarah Sulzer-Mosse, Fredrik Cedarbaum, Jayant Umarye, Ravindra Sonawane
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Publication number: 20150031678Abstract: The present invention relates to new substituted pyrazolo[1,5-a]pyridine having a great affinity for sigma receptors, especially sigma-1 receptor, as well as to the process for the preparation thereof, to compositions comprising them, and to their use as medicaments.Type: ApplicationFiled: February 21, 2013Publication date: January 29, 2015Applicant: LABORATORIES DEL DR. ESTEVE S.A.Inventors: José Luis Diaz Fernández, Ma Rosa Cuberes Altisent
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Publication number: 20150031668Abstract: Chroman compounds and derivatives of Formula I are useful inhibitors of TRPM8. Such compounds are useful in treating a number of TRPM8 mediated disorders and conditions and may be used to prepare medicaments and pharmaceutical compositions useful for treating such disorders and conditions. Examples of such disorders include, but are not limited to, migraines and neuropathic pain. Compounds of Formula I have the following structure: where the definitions of the variables are provided herein.Type: ApplicationFiled: July 15, 2014Publication date: January 29, 2015Inventors: Kaustav Biswas, Jian J. Chen, Vijay Keshav Gore, Scott Harried, Daniel B. Horne, Matthew R. Kaller, Vu Van Ma, Kelvin Sham, James Brown, Wenge Zhong, Thomas T. Nguyen
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Publication number: 20150031716Abstract: The present invention is directed to piperidinone carboxamide indane derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. 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 CGRP is involved.Type: ApplicationFiled: October 2, 2014Publication date: January 29, 2015Inventors: Ian M. Bell, Mark E. Fraley, Steven N. Gallicchio, Anthony Ginnetti, Helen J. Mitchell, Daniel V. Paone, Donnette D. Staas, Cheng Wang, C. Blair Zartman, Heather E. Stevenson
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Patent number: 8940737Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-xL protein.Type: GrantFiled: October 11, 2012Date of Patent: January 27, 2015Assignee: AbbVie Inc.Inventors: Le Wang, George Doherty, Xilu Wang, Zhi-Fu Tao, Milan Bruncko, Aaron R. Kunzer, Michael D. Wendt, Xiaohong Song, Robin Frey, Todd M. Hansen, Gerard M. Sullivan, Andrew Judd, Andrew Souers
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Publication number: 20150025041Abstract: Disclosed are methods of treating viral infections comprising, in one aspect, administering compounds that are phospholipase D inhibitors. 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. In accordance with the purpose(s) of the invention, as embodied and broadly described herein, the invention, in one aspect, relates to antiviral therapies. For example, compounds having Phospholipase D activity (e.g., isoform selective Phospholipase D inhibitors) can be useful in antiviral therapies (e.g., influenza treatments).Type: ApplicationFiled: September 30, 2012Publication date: January 22, 2015Applicant: VANDERBILT UNIVERSITYInventors: Craig W. Lindsley, H. Alex Brown
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Publication number: 20150025098Abstract: The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof; wherein G is R1, R2 and R3 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.Type: ApplicationFiled: September 26, 2014Publication date: January 22, 2015Applicant: PFIZER INC.Inventors: David A. Griffith, Robert L. Dow, Scott W. Bagley, Aaron Smith
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Publication number: 20150025012Abstract: Provided herein are methods, assays and kits for evaluating a sample, e.g., a sample obtained from a cancer patient, to detect one or more hedgehog biomarkers and/or one or more cilium markers. Thus, the invention can be used, inter alia, as a means to identify patients likely to benefit from administration of one or more hedgehog inhibitors, alone or in combination with therapeutic agents; to predict a time course of disease or a probability of a significant event in the disease of a cancer patient; to stratify patient populations; and/or to more effectively treat or prevent a cancer or a tumor associated with hedgehog signaling.Type: ApplicationFiled: August 8, 2014Publication date: January 22, 2015Inventors: John R. MacDougall, Juan Guillermo Paez, Karen J. McGovern, Jeffery L. Kutok, Georgios Skliris, Kerry White, Kerrie L. Faia, Marisa Osswalt Peluso, Veronica Travaglione Campbell
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Publication number: 20150018339Abstract: Compounds having the general formula II, III, or IV wherein R1 can be a radical of an optionally substituted C-4 to C-7 N-containing heterocycle or a radical of an optionally substituted cyclic or acyclic tertiary amine or isoindoline-1,3-dione: R2,3,4,5,6 can each independently be any one or combinations of the following moieties, cyano, nitro, acyl, alkyl, amido, azido, isothiocyanate, isocyanate, optionally substituted anilino, halogens, ethers, sulfonamides, thioacyl, nitro, aromatic, heterocyclic, olefinic, acetylene, deuterium, or tritium; Y can be either CH, CH2, O, S, OCH2, N—R, N—Ar, C—R, C—Ar; Z can be either H, O, S, S—R or NR.Type: ApplicationFiled: February 21, 2014Publication date: January 15, 2015Inventors: Christopher R. MCCURDY, Christophe Mesangeau, Bonnie Ann Avery, Ahmed Hassan Amin Abdelazeem, Frederick T. Chin, Jacques Henri Poupaert
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Publication number: 20150017651Abstract: Methods and composition for tumor therapy, especially esophageal adenocarcinoma (EAC), are described. For example, in certain aspects methods for determining Hedgehog and mTOR signaling pathway status to select patients for administering a combination therapy of Hedgehog and mTOR signaling inhibitors are described. Furthermore, the invention provides compositions that involve testing kits for determining signaling status.Type: ApplicationFiled: January 14, 2013Publication date: January 15, 2015Applicant: Board of Regents, The University of Texas SystemInventors: Mien-Chie Hung, Yan Wang, Jaffer Ajani
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Publication number: 20150018347Abstract: The present application describes modulators of chemokine receptor activity of formula I or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and transplant rejection using modulators of formula (I) are disclosed.Type: ApplicationFiled: October 1, 2014Publication date: January 15, 2015Inventors: T. G. Murali Dhar, John V. Duncia, Daniel S. Gardner, Weiwei Guo, John Hynes
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Publication number: 20150018269Abstract: The invention relates to compounds that can be used, in particular, as structural mimetics of proline-rich peptides and are correspondingly able to bond with proline-rich-motif binding domains (PRM domains) of proteins. The invention further relates to the use of these compounds as pharmaceutically active agents, as well as the use of the pharmaceutically active agents for the treatment of bacterial, neurodegenerative and tumor diseases.Type: ApplicationFiled: August 24, 2012Publication date: January 15, 2015Applicants: UNIVERSITÄT ZU KÖLN, FORSCHUNGSVERBUND BERLIN E.V.Inventors: Ronald Kühne, Hartmut Oschkinat, Robert Opitz, Matthias Müller, Hans-Günther Schmalz, Cedric Reuter, Peter Huy
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Publication number: 20150018377Abstract: The invention provides a compound of formula (Ia), and pharmaceutically acceptable salts thereof. The invention also provides use of the compounds or salts as modulators of Kv3.1 and/or Kv3.2, and in the treatment of diseases or disorders where a modulator of Kv3.1 and/or Kv3.2 is required, such as depression and mood disorders, hearing disorders, schizophrenia, substance abuse disorders, sleep disorders or epilepsy.Type: ApplicationFiled: March 27, 2014Publication date: January 15, 2015Applicant: AUTIFONY THERAPEUTICS LIMITEDInventors: Giuseppe ALVARO, Anne Decor, Stefano Fontana, Dieter Hamprecht, Charles Large, Agostino Marasco
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Patent number: 8933074Abstract: 1,2-disubstituted heterocyclic compounds which are inhibitors of phosphodiesterase 10 are described. Also described are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function. Among the disorders which may be treated are neurological, neurodegenerative and psychiatric disorders including, but not limited to, those associated with cognitive deficits or schizophrenic symptoms.Type: GrantFiled: June 17, 2013Date of Patent: January 13, 2015Assignee: FORUM Pharmaceuticals Inc.Inventors: Amy Ripka, Gideon Shapiro, Richard Chesworth
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Publication number: 20150011470Abstract: The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt of the compound, wherein R1, R2, R3, Z, A1, L and A2 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.Type: ApplicationFiled: September 19, 2014Publication date: January 8, 2015Applicant: PFIZER INC.Inventors: Mary Theresa Didiuk, Robert Lee Dow, David Andrew Griffith
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Publication number: 20150011532Abstract: Compounds having the following formula: wherein A is, or; and X is N or C—R7, or an enantiomer, diastereomer or a pharmaceutically-acceptable salt thereof, are useful as kinase modulators, including IRAK-4 modulation.Type: ApplicationFiled: January 11, 2013Publication date: January 8, 2015Inventors: Venkatram Reddy Paidi, Sreekantha Ratna Kumar, Abhisek Banejee, Ramesh Sistla, Satheesh Kesavan Nair, William J. Pitts, John Hynes
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Patent number: 8927534Abstract: The present invention is related to a compound of formula (I), wherein A is a nonaromatic heterocyclic ring, Ar is either absent or phenylene; ? is a radical of formula (II), R2 is a hydrophobic moiety; and G is a radical containing one or more moieties selected from the group consisting of NH, OH and a basic moiety. The compounds are inhibitors of integrins, especially antagonists of the fibronectin receptor alpha5beta1, useful as anti-angiogenic agents.Type: GrantFiled: January 31, 2007Date of Patent: January 6, 2015Assignee: Shire Orphan Therapies GmbHInventors: Gunther Zischinsky, Roland Stragies, Frank Osterkamp, Dirk Scharn, Gerd Hummel, Holger Kalkhof, Grit Zahn, Doerte Vossmeyer, Claudia Christner-Albrecht, Ulrich Reineke
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Patent number: 8927715Abstract: This invention relates to novel compounds of the Formula (I*), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of Cortisol in a cell or the inhibition of the conversion of cortisone to Cortisol in a cell.Type: GrantFiled: August 24, 2007Date of Patent: January 6, 2015Assignee: Vitae Pharmaceuticals, Inc.Inventors: David A. Claremon, Suresh B. Singh, Colin M. Tice, Yuanjie Ye, Salvacion Cacatian, Wei He, Robert Simpson, Zhenrong Xu, Wei Zhao
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Publication number: 20150005319Abstract: The invention relates generally to macrocyclic compounds of formula I and their therapeutic use. More particularly, the invention relates to macrocyclic compounds that modulate the activity of IL-17 and/or are useful in the treatment of medical conditions, such as inflammatory diseases and other IL-17-associated disorders.Type: ApplicationFiled: February 1, 2013Publication date: January 1, 2015Inventors: Michael Taylor, Nicholas K. Terrett, William H. Connors, Cheri Snedeker, Kelley C. Shortsleeves, Benjamin A. Seigal, Stephen P. Hale, Timothy F. Briggs, Frank G. Favaloro, Jr., Tyler J. Cipriani, Dingxue Yan, Sethu L. Alexander, Atli Thorarensen, Li Xing
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Publication number: 20150005304Abstract: The invention relates to pyran spirocyclic piperidine amide compounds useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: ApplicationFiled: January 15, 2013Publication date: January 1, 2015Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Sara Sabina Hadida-Ruah, Vijayalaksmi Arumugam, Michael Paul Deninno, Bryan A. Frieman, Edward Adam Kallel, Mark Thomas Miller, Johnny Uy, Jinglan Zhou
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Publication number: 20150005163Abstract: A pesticidal mixture comprising as active ingredient a mixture of component A and component B, wherein component A is a compound of formula (I) in which Q is i or ii wherein X, Y and Z, m and n, A, G, and R, are as defined as in claim 1, and component B is a compound selected from the insecticides as defined in claim 1. The present invention also relates to methods of using said mixtures for the control of plant pests.Type: ApplicationFiled: January 17, 2013Publication date: January 1, 2015Applicant: SYNGENTA PARTICIPATIONS AGInventors: Anke Buchholz, Fabienne Hatt, Alfred Rindlisbacher, Michel Muehlebach
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Publication number: 20150005330Abstract: The present invention is directed to piperidinone carboxamide azaindane derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. 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 CGRP is involved.Type: ApplicationFiled: September 12, 2014Publication date: January 1, 2015Inventors: Ian M. Bell, Mark E. Fraley, Steven N. Gallicchio, Anthony Ginnetti, Helen J. Mitchell, Daniel V. Paone, Donnette D. Staas, Cheng Wang, C. Blair Zartman
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Publication number: 20150005162Abstract: A pesticidal mixture comprising as active ingredient a mixture of component A and component B, wherein component A is a compound of formula (I), in which Q is i or ii wherein X, Y and Z, m and n, A, G, and R, are as defined as in claim 1, and component B is a compound selected from the insecticides as defined in claim 1. The present invention also relates to methods of using said mixtures for the control of plant pests.Type: ApplicationFiled: January 17, 2013Publication date: January 1, 2015Applicant: Syngenta Participations AGInventors: Anke Buchholz, Fabienne Hatt, Alfred Rindlisbacher, Michel Muehlebach
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Patent number: 8921555Abstract: The present invention relates to substituted 1,3,8-triazaspiro[4.5]decame-2,4-diones useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.Type: GrantFiled: June 7, 2010Date of Patent: December 30, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Joan M. Pierce, Jeffrey J. Hale, Shouwu Miao, Petr Vachal
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Patent number: 8921576Abstract: The present invention provides a novel compound represented by a general formula (1) as shown below, which has a glucokinase-activating action in the liver and pancreatic ?-cells and which is useful as an agent for preventing and/or treating diseases caused by hyperglycemia, such as diabetes. A spiroindoline compound represented by the general formula (1), or a salt thereof, or a solvate of the compound or the salt: [wherein ring A represents a nitrogen-containing 5-10 membered heteroaryl group; R1 and R2, which are the same or different, each represent a hydrogen atom, a halogen atom, a halo C1-6 alkyl group, a C6-10 aryl group, a cyano group, a C1-6 alkyl group optionally having a substituent, a C2-6 alkenyl group optionally having a substituent, etc.; R3 represents a hydrogen atom, a C1-6 alkyl group optionally having a substituent, etc.; and R4 represents a hydrogen atom, a halogen atom, a C1-6 alkyl group optionally having a substituent, etc.Type: GrantFiled: October 18, 2012Date of Patent: December 30, 2014Assignee: Kowa Company, Ltd.Inventors: Takahisa Ogamino, Yukiyoshi Yamazaki, Shin Tanikawa, Ayumu Okuda, Tomoaki Fukuda, Okihisa Tokuda, Yoshiharu Miyake, Shinsuke Itoh, Hiroyuki Ishiwata
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Patent number: 8921359Abstract: The present invention is directed to a compound represented by the following structural formula: or a pharmaceutically acceptable salt thereof. Pharmaceutical composition comprising a compound represented by Structural Formula (I) and method of use of these compound for inhibiting BACE activity in a subject in need of such treatment are also described.Type: GrantFiled: April 22, 2013Date of Patent: December 30, 2014Assignee: Vitae Pharmaceuticals, Inc.Inventors: Lawrence W. Dillard, Jing Yuan, Lanqi Jia, Yajun Zheng
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Patent number: 8921363Abstract: The present invention relates to a compound represented by general formula I: or a stereoisomer, tautomer, hydrate, solvate or pharmaceutically acceptable salt thereof, wherein A1, A2, A3, A4, A5, A6, R2, R7, W, X, Y and Z are defined within. These compounds are useful for the modulation of ?-secretase enzyme activity and for the treatment of ?-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions.Type: GrantFiled: August 4, 2011Date of Patent: December 30, 2014Assignee: Amgen Inc.Inventors: Ana Elena Minatti, Yuan Cheng, Wenge Zhong
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Publication number: 20140378473Abstract: This invention relates to novel diarylamino compounds that bind to the sigma-2 receptor, to pharmaceutical compositions comprising such compounds, and to methods for inhibiting or restoring synapse loss in neuronal cells, modulating a membrane trafficking change in neuronal cells, and treating cognitive decline and neurodegenerative diseases and disorders therewith.Type: ApplicationFiled: August 27, 2012Publication date: December 25, 2014Applicant: COGNITION THERAPEUTICS, INC.Inventors: Susan M. Catalano, Gilbert Rishton, Nicholas J. Izzo
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Publication number: 20140378430Abstract: The present invention relates to heterocyclic compounds useful for antagonising angiotensin II Type 2 (AT2) receptor. More particularly the invention relates to pyrrolidine and azetidine compounds, compositions containing them and their use in methods of treating or preventing disorders or diseases associated with AT2 receptor function including neuropathic pain, inflammatory pain, conditions associated with neuronal hypersensitivity, impaired nerve conduction velocity, cell proliferation disorders, disorders associated with an imbalance between bone resorption and bone formation and disorders associated with aberrant nerve regeneration.Type: ApplicationFiled: January 4, 2013Publication date: December 25, 2014Applicant: SPINIFEX PHARMACEUTICALS PTY LTDInventors: Thomas David McCarthy, Alan Naylor