Bicyclo Ring System Having The Diazine Ring As One Of The Cyclos Patents (Class 544/349)
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Publication number: 20140221357Abstract: The present invention provides compounds of Formula (I) or Formula (III): [INSERT CHEMICAL STRUCTURE HERE] (I) [INSERT CHEMICAL STRUCTURE HERE] (III) as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.Type: ApplicationFiled: September 25, 2012Publication date: August 7, 2014Applicant: Bristol-Myers Squibb CompanyInventors: Lynn Abell, Leonard Adam, Cullen L. Cavallaro, Heather Finlay, Todd J. Friends, Jon J. Hangeland, Ji Jiang, R. Michael Lawrence, John Lloyd, Zulan Pi, George O. Tora, Jennifer X. Qiao, Carol Hui Hu, Tammy C. Wang
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Patent number: 8796257Abstract: A compound of formula (I): wherein: M is hydrogen or a pharmaceutically acceptable salt-forming cation; Y is OR1 or NR2R3, and R1, R2, R3 and M are as defined herein. Also, methods of treating bacterial infection, pharmaceutical compositions, molecular complexes and processes for preparing compounds.Type: GrantFiled: November 30, 2012Date of Patent: August 5, 2014Assignee: Naeja Pharmaceutical Inc.Inventors: Samarendra N. Maiti, Dai Nguyen, Jehangir Khan, Rong Ling
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Patent number: 8796454Abstract: Herein we describe compositions and methods for the synthesis of [2.2.2]-diazabicyclic structures comprising a domino reaction sequence involving aldol condensation, alkene isomerization, and intramolecular hetero-Diels-Alder cycloaddition. Excellent diastereofacial control during the cycloaddition is enforced with a removable chiral phenyl aminal diketopiperazine substituent. The reaction sequence rapidly generates molecular complexity and is competent with both enolizable and non-enolizable aldehyde substrates. This method provides an efficient route to [2.2.2]-diazabicyclic structures, common to bioactive prenylated indole alkaloids such as the brevianamides and stephacidins.Type: GrantFiled: May 1, 2013Date of Patent: August 5, 2014Assignee: College of William and MaryInventor: Jonathan R. Scheerer
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Patent number: 8791117Abstract: Embodiments of this invention provide methods for therapeutic use of cyclic G-2-Allyl Proline to treat cognitive disorders as well as manufacture of medicaments including tablets, capsules, injectable solutions that are useful for treatment of such conditions.Type: GrantFiled: March 8, 2011Date of Patent: July 29, 2014Assignee: Neuren Pharmaceuticals LimitedInventors: Michael John Bickerdike, Jian Guan
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Patent number: 8791119Abstract: Compounds corresponding to the general formula (I) wherein R2 represents a group C1-10-alkyl, C3-10-cycloalkyl, C3-7-cycloalkyl-C1-6-alkyl, C1-6-alkyl-C3-7-cycloalkyl, C3-7-cycloalkyl-C3-7-cycloalkyl, C1-6-alkylthio-C-1-10-alkyl, C1-6-alkoxy-C1-10-alkyl, hydroxy-C1-10-alkyl, hydroxy-C1-6-alkyl-C3-7-cycloalkyl-C1-6-alkyl, hydroxy-C3-10-cycloalkyl, C1-10-fluoroalkyl or C3-10-fluorocycloalkyl; an optionally substituted heterocyclic group; a group C1-10-alkyl substituted with an optionally substituted heterocyclic group; X6 represents a group chosen from hydrogen, fluorine, chlorine and bromine atoms or a group C1-6-alkyl, C3-7-cycloalkyl, C3-7-cycloalkyl-C1-6-alkyl, C1-6-fluoroalkyl or cyano; and R7 represents an aryl group such as phenyl or naphthyl, optionally substituted with one or more substituents, in the form of the base or of an acid-addition salt, and the therapeutic use thereof.Type: GrantFiled: November 29, 2012Date of Patent: July 29, 2014Assignee: SanofiInventors: Sylvain Cote Des Combes, Jacques Froissant, Jean-Francois Gibert, Frank Marguet, Christophe Pacaud, Frédéric Puech, Antoine Ravet
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Publication number: 20140206680Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein G, p, R1, R2, R3a, R4, and R5 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating disorders, diseases, and conditions involving the immune system and inflammation, including rheumatoid arthritis, cancer, and other disorders, diseases, and conditions for which inhibition of SYK is indicated.Type: ApplicationFiled: June 20, 2012Publication date: July 24, 2014Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Mark E. Adams, Rongliang Chen, Mitsunori Kono, Betty Lam, Matthew Lardy, Srinivasa Reddy Natala, Steven James Wilkens, Zhe Nie
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Publication number: 20140200209Abstract: The present invention is to provide a novel compound (I) shown below, having the anti-virus activity; particularly the HIV integrase inhibitory activity, and a drug containing the same, particularly an anti-HIV drug, as well as a process and an intermediate thereof. (wherein Z1 is NR4; R1 is hydrogen or lower alkyl; X is a single bond, a hetero atom group selected from O, S, SO, SO2 and NH, or lower alkylene or lower alkenylene in which the hetero atom group may intervene; R2 is optionally substituted aryl; R3 is hydrogen, a halogen, hydroxy, optionally substituted lower alkyl etc; and R4 and Z2 part taken together forms a ring, to form a polycyclic compound, including e.g., a tricyclic or tetracyclic compound.Type: ApplicationFiled: March 14, 2014Publication date: July 17, 2014Applicants: ViiV Healthcare Company, Shionogi & Co., Ltd.Inventors: Brian A. JOHNS, Takashi KAWASUJI, Teruhiko TAISHI, Yoshiyuki TAODA
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Publication number: 20140194418Abstract: Compounds of formula (I) or pharmaceutical acceptable salts are provided, wherein X1˜X5, R1˜R3, A, B, Z and n are defined in the description. And compositions containing said compounds, and the uses for inhibitors of kinases such as ALK, and the uses for treating cancer thereof are provided.Type: ApplicationFiled: January 20, 2012Publication date: July 10, 2014Applicant: ABBVIE INC.Inventors: Anil Vasudevan, Thomas Dale Penning, Huanming Chen, Bo Liang, Shaohui Wang, Fengchun Wu, Yan Shen, Cuihua Liu, Zhenguang Zou, Marina Pliushchev
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Publication number: 20140186951Abstract: Certain quinolizidine and octahydropyridopyrazine compounds, pharmaceutical compositions, and methods of their use, inter alia, as opioid receptor antagonists are disclosed.Type: ApplicationFiled: March 10, 2014Publication date: July 3, 2014Applicant: Adolor CorporationInventors: Roland E. Dolle, Bertrand Le Bourdonnec, Allan James Goodman
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Patent number: 8765921Abstract: There has been a need for coelenterazine analogs that exhibit luminescence properties different from those of known coelenterazine analogs. The present invention provides the compound represented by general formula (1).Type: GrantFiled: August 22, 2013Date of Patent: July 1, 2014Assignees: JNC Corporation, Tokyo Institute of TechnologyInventors: Satoshi Inouye, Yuiko Sahara, Rie Iimori, Takamitsu Hosoya
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Publication number: 20140179672Abstract: The present application relates to novel substituted imidazo[1,2-a]pyridine-3-carboxamides, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.Type: ApplicationFiled: November 1, 2013Publication date: June 26, 2014Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Alexandros VAKALOPOULOS, Markus FOLLMANN, Ingo HARTUNG, Philipp BUCHGRABER, Rolf JAUTELAT, Jorma HAßFELD, Niels LINDNER, Alexey GROMOV, Frank WUNDER, Johannes-Peter STASCH, Gorden REDLICH, Volkhart Min-Jian LI, Eva Maria BECKER-PELSTER, Andreas KNORR
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Publication number: 20140162998Abstract: A Pim kinase inhibitor compound having the structure represented by Formula I, and isomers, diastereomers, enantiomers, tautomers, and pharmaceutically acceptable salts thereof. The compounds significantly inhibit Pim kinase activity and can be used to prepare drugs for treating Pim kinase mediated diseases, such as cancers, autoimmune diseases, allergic reactions, or organ transplant rejection. Also provided are methods for preparing the compounds represented by Formula I.Type: ApplicationFiled: February 10, 2014Publication date: June 12, 2014Applicant: Jikai Biosciences, Inc.Inventor: Yu GE
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Publication number: 20140163009Abstract: Provided are certain histone deacetylase (HDAC) inhibitors of Formula I, compositions thereof, and methods of their use.Type: ApplicationFiled: January 23, 2012Publication date: June 12, 2014Applicant: CHDI FoundationInventors: Christopher A Luckhurst, Alen F Haughan, Perla Breccia, Andrew J Stott, Roland W Burli, Samantha J Hughes, Ignacio Munoz-Sanjuan, Celia Dominguez
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Patent number: 8748429Abstract: The disclosure generally relates to the novel compounds of formula I, including pharmaceutically acceptable salts, which are CGRP receptor antagonists. The disclosure also relates to pharmaceutical compositions and methods for using the compounds in the treatment of CGRP related disorders including migraine and other headaches, neurogenic vasodilation, neurogenic inflammation, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases such as asthma, and chronic obstructive pulmonary disease (COPD).Type: GrantFiled: April 4, 2012Date of Patent: June 10, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Guanglin Luo, Gene M. Dubowchik, John E. Macor, Ling Chen
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Publication number: 20140154179Abstract: Compounds having formula I, or pharmaceutically acceptable salts, hydrates or N-oxides thereof are provided and are useful for binding to CXCR7, and treating diseases that are dependent, at least in part, on CXCR7 activity. Accordingly, the present invention provides in further aspects, compositions containing one or more of the above-noted compounds in admixture with a pharmaceutically acceptable excipient.Type: ApplicationFiled: November 27, 2013Publication date: June 5, 2014Applicant: ChemoCentryx, Inc.Inventors: Junfa Fan, Antoni Krasinski, Christopher W. Lange, Rebecca M. Lui, Jeffrey P. McMahon, Jay P. Powers, Yibin Zeng, Penglie Zhang
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Publication number: 20140155393Abstract: The present invention relates to novel triazolo[4,3-a]pyridine derivatives of Formula (I) wherein all radicals are as defined in the claims. The compounds according to the invention are positive allosteric modulators of the metabotropic glutamate receptor subtype 2 (“mGluR2”), which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, and to the use of such compounds for the prevention or treatment of neurological and psychiatric disorders and diseases in which mGluR2 is involved.Type: ApplicationFiled: November 8, 2011Publication date: June 5, 2014Applicant: Janssen Pharmaceuticals, Inc.Inventors: José Maria Cid-Núñez, Andrés Avelino Trabanco-Suárez, Juan Antonio Vega Ramiro, Daniel Oehlrich, Gary John Tresadern, Gregor James Macdonald
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Publication number: 20140155387Abstract: The present invention refers to: a compound having the general formula (I), wherein n is 0, 1, 2 or; m is 0, 1, 2 or 3; o is 0, 1, 2 or 3; W, X, Y and Z are independently selected from CH, N or N-oxide; A is NR4, C?O, C?S, OP(O)(O), P?O, CH2, or a heteroarly selected from the group consisting of (a), (b), (c), (d), (e), (f), (g); V is C?O, O, S, CH2, or NR5; as well as its use in treating inflammatory diseases such as asthma, COPD, inflammation post infection, arthritis, atherosclerosis, pain and dermatitis.Type: ApplicationFiled: April 20, 2012Publication date: June 5, 2014Applicants: QURIENT, CO. LTD., INSTITUT PASTEUR KOREAInventors: Zaesung No, Jaeseung Kim, Sung-Jun Han, Jung Hwan Kim, Young Sam Park, Sangchul Lee, Kiyean Nam, Jeongjun Kim, Jinhwa Lee, Sunhee Kang, Min Jung Seo, Saeyeon Lee, Gahee Choi
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Patent number: 8741491Abstract: Embodiments are related to ionic liquids and more specifically to ionic liquids used in electrochemical metal-air cells in which the ionic liquid includes sulfonate ions as the anion.Type: GrantFiled: April 17, 2012Date of Patent: June 3, 2014Assignee: Fluidic, Inc.Inventors: Derek Wolfe, Cody A. Friesen, Paul Bryan Johnson
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Patent number: 8741899Abstract: The present application relates to calcium channel inhibitors comprising compounds of formula (I), formula (II), formula (III), or formula (IV), wherein L1, R1, R2, R3, R4, R5, R6, R7 and Rc are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.Type: GrantFiled: February 4, 2013Date of Patent: June 3, 2014Assignee: AbbVie Inc.Inventors: Qingwei Zhang, Andrew O. Stewart, Zhiren Xia
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Publication number: 20140148599Abstract: A P2X4 receptor antagonist such as paroxetine, a diazepinedione derivative having the following formula (IX) is used as an agent for preventing or treating zoster-associated pain in acute phase: wherein R1 is hydrogen, a C1-8 alkyl group, or the like; each of R2 and R3 is hydrogen, a C1-8 alkyl group, or the like; each of R4 and R5 is hydrogen or the like; and W is a five-membered or six-membered heterocyclic ring optionally having one or more substituents and comprising one to four nitrogen atoms as the members of the ring.Type: ApplicationFiled: November 2, 2011Publication date: May 29, 2014Applicants: NIPPON CHEMIPHAR CO., LTD., KYUSHU UNIVERSITYInventors: Kazuhide Inoue, Makoto Tsuda, Yuta Matsumura
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Publication number: 20140142114Abstract: The present invention relates to novel anthelmintic compounds of formula (I) below: wherein Y and Z are independently a bicyclic carbocyclic or a bicyclic heterocyclic group, or one of Y or Z is a bicyclic carbocyclic or a bicyclic heterocyclic group and the other of Y or Z is alkyl, alkenyl, alkynyl, cycloalkyl, phenyl, heterocyclyl or heteroaryl, and variables X1, X2, X3, X4, X5, X6, X7 and X8 are as defined herein. The invention also provides for veterinary compositions comprising the anthelmintic compounds of the invention, and their uses for the treatment and prevention of parasitic infections in animals.Type: ApplicationFiled: November 19, 2013Publication date: May 22, 2014Applicant: Merial LimitedInventors: Charles Q. Meng, Alan Long, Scot Huber, Srinivas Reddy Gurrala, Douglas Edward Wilkinson, Gregory Pacofsky
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Patent number: 8697697Abstract: This invention describes substituted pyrazole derivatives of Formula I and methods of making and using the compounds. These compounds have utility in the treatment of conditions or diseases in which modification of the activity of ERK would have a positive therapeutic outcome, for instance various cancers, psoriasis and actinic keratosis.Type: GrantFiled: January 3, 2012Date of Patent: April 15, 2014Assignee: Kinentia Biosciences LLCInventors: David Fairfax, Russell Joseph Deorazio
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Patent number: 8697673Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I as defined herein. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.Type: GrantFiled: March 29, 2012Date of Patent: April 15, 2014Assignee: Pfizer Inc.Inventors: Martin Youngjin Pettersson, Douglas Scott Johnson, Chakrapani Subramanyam, Christopher John O'Donnell, Christopher William am Ende, Benjamin Adam Fish, Michael Eric Green, Patrick Bradley Mullins, Cory Michael Stiff, Tuan Phong Tran, Thayalan Navaratnam
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Publication number: 20140088111Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.Type: ApplicationFiled: September 19, 2013Publication date: March 27, 2014Applicant: Pfizer Inc.Inventors: Martin Youngjin Pettersson, Douglas Scott Johnson, Chakrapani Subramanyam, Christopher John O'Donnell, Christopher William am Ende, Michael Eric Green, Nandini Chaturbhai Patel, Cory Michael Stiff, Tuan Phong Tran, Gregory Wayne Kauffman, Antonia Friederike Stepan, Patrick Robert Verhoest
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Patent number: 8673920Abstract: This invention relates to compounds having structural Formula I: and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds of Formula I are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.Type: GrantFiled: April 27, 2010Date of Patent: March 18, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Alexander Pasternak, Aurash Shahripour, Haifeng Tang, Nardos H. Teumelsan, Lihu Yang, Yuping Zhu, Shawn P. Walsh
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Patent number: 8669255Abstract: The present application relates to: (a) compounds of Formula (I): and salts thereof, wherein Z1, Z2, Z3, Z4, R1, R2, and R3 are as defined in the specification; (b) compositions comprising such compounds and salts; and (c) methods of use of such compounds, salts, and compositions, particularly use as calcium channel inhibitors.Type: GrantFiled: September 26, 2012Date of Patent: March 11, 2014Assignee: AbbVie Inc.Inventors: Tao Li, Sachin V. Patel, Richard J. Perner, John T. Randolph, Michael R. Schrimpf, Kevin R. Woller, Zhiren Xia, Qingwei Zhang
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Publication number: 20140066369Abstract: The present invention relates to compounds of Formula I and pharmaceutically acceptable salts, solvates, and hydrates thereof, that are useful as single pharmaceutical agents or in combination with one or more additional pharmaceutical agents, such as, a DPP-IV inhibitor, a biguanide, an alpha-glucosidase inhibitor, an insulin analogue, a sulfonylurea, an SGLT2 inhibitor, a meglitinide, a thiazolidinedione, or an anti-diabetic peptide analogue, in the treatment of for example, a disorder selected from: a GPR119-receptor-related disorder; a condition ameliorated by increasing a blood incretin level; a condition characterized by low bone mass; a neurological disorder; a metabolic-related disorder; type 2 diabetes; obesity; and complications related thereto.Type: ApplicationFiled: April 18, 2012Publication date: March 6, 2014Applicant: ARENA PHARMACEUTICALS, INC.Inventors: Robert M. Jones, Daniel J. Buzard, Sangdon Han, Sun Hee Kim, Juerg Lehmann, Dawei Yue, Xiuwen Zhu
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Patent number: 8658569Abstract: Substituted quinolinones of the formula I in which the variables are defined according to the description, their agriculturally suitable salts, processes and intermediates for preparing the compounds of the formula I, compositions comprising them and their use as herbicides, i.e. for controlling harmful plants, and also a method for controlling unwanted vegetation which comprises allowing a herbicidally effective amount of at least one compound of the formula I to act on plants, their seed and/or their habitat.Type: GrantFiled: August 22, 2012Date of Patent: February 25, 2014Assignee: BASF SEInventors: Dschun Song, Julia Major, Johannes Hutzler, Trevor William Newton, Matthias Witschel, William Karl Moberg, Liliana Parra Rapado, Tao Qu, Frank Stelzer, Andree Van Der Kloet, Thomas Seitz, Thomas Ehrhardt, Klaus Kreuz, Klaus Grossmann, Anna Aleksandra Michrowska, Anja Simon, Richard Roger Evans
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Patent number: 8658635Abstract: The invention is directed to certain novel compounds of formula (I) and salts thereof. The compounds of the invention are inhibitors of PI3-kinase activity.Type: GrantFiled: June 3, 2009Date of Patent: February 25, 2014Assignee: GlaxoSmithKline Intellectual Property Development LimitedInventors: Ian Robert Baldwin, Kenneth David Down, Paul Faulder, Simon Gaines, Julie Nicole Hamblin, Joelle Le, Christopher James Lunniss, Nigel James Parr, Timothy John Ritchie, John Edward Robinson, Juliet Kay Simpson, Christian Alan Paul Smethurst
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Patent number: 8653260Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.Type: GrantFiled: June 20, 2012Date of Patent: February 18, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Richard Berger, Lehua Chang, Scott D. Edmondson, Stephen D. Goble, Sookhee Nicole Ha, Nam Fung Kar, Ihor E. Kopka, Bing Li, Gregori J. Morriello, Chris R. Moyes, Ding-Ming Shen, Liping Wang, Cheng Zhu
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Patent number: 8653263Abstract: Disubstituted octahydropyrrolo[3,4-c]pyrrole compounds are described, which are useful as orexin receptor modulators. Such compounds may be useful in pharmaceutical compositions and methods for the treatment of diseased states, disorders, and conditions mediated by orexin activity, such as insomnia.Type: GrantFiled: October 21, 2010Date of Patent: February 18, 2014Assignee: Janssen PharmaceuticaInventors: Wenying Chai, Michael A. Letavic, Kiev S. Ly, Daniel J. Pippel, Dale A. Rudolph, Kathleen C. Sappey, Brad M. Savall, Chandravadan R. Shah, Brock T. Shireman, Akinola Soyode-Johnson, Emily M. Stocking, Devin M. Swanson
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Publication number: 20140045790Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I as defined herein. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.Type: ApplicationFiled: October 15, 2013Publication date: February 13, 2014Applicant: Pfizer Inc.Inventors: Martin Youngjin Pettersson, Douglas Scott Johnson, Chakrapani Subramanyam, Christopher John O'Donnell, Christopher William am Ende, Benjamin Adam Fish, Michael Eric Green, Patrick Bradley Mullins, Cory Michael Stiff, Tuan Phong Tran, Thayalan Navaratnam
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Patent number: 8648074Abstract: The present application relates to: (a) compounds of Formula (I): and salts thereof, wherein Z?, Z?, L2, G2, R1, and R2 are as defined in the specification; (b) compositions comprising such compounds and salts; and (c) methods of use of such compounds, salts, and compositions, particularly use as calcium channel blockers.Type: GrantFiled: September 26, 2012Date of Patent: February 11, 2014Assignee: AbbVie Inc.Inventors: Tao Li, Sachin V. Patel, Richard J. Perner, John T. Randolph, Michael R. Schrimpf, Kevin R. Woller, Zhiren Xia, Qingwei Zhang
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Patent number: 8648070Abstract: This invention relates to bicyclic ring system substituted sulfonamide functionalized phenols of general formula 1, their use as inhibitors of CXCR2 activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin, or eyes, diseases of the peripheral or central nervous system or cancers, as well as pharmaceutical compositions which contain these compounds.Type: GrantFiled: December 13, 2011Date of Patent: February 11, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Riccardo Giovannini, Dieter Hamprecht, Barbara Kistler, Iain Lingard
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Publication number: 20140038946Abstract: The disclosure relates to (heterocycle-fused piperidine)-(piperazinyl)-1-alkanone derivatives and (heterocycle-fused pyrrolidine)-(piperazinyl)-1-alkanone derivatives of formula (I): wherein A, W, R2 and n are as defined in the disclosure, to the method of preparation thereof and the therapeutic use thereof.Type: ApplicationFiled: October 8, 2013Publication date: February 6, 2014Applicant: SANOFIInventors: Marco BARONI, Francoise BONO, Sandrine DELBARY-GOSSART, Valentina VERCESI
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Publication number: 20140031339Abstract: The present invention relates to compounds of formula (I): or a pharmaceutically acceptable salt thereof, wherein A1, A2, L1 and B are as defined herein. The compounds of formula (I) are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorders. The present invention also relates to pharmaceutical compositions comprising the compounds of formula (I), methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.Type: ApplicationFiled: July 16, 2013Publication date: January 30, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Asitha ABEYWARDANE, Steven Richard BRUNETTE, Michael Jason BURKE, Thomas Martin KIRRANE, JR., Chuk Chui MAN, Daniel Richard MARSHALL, Anil Kumar PADYANA, Hossein RAZAVI, Robert SIBLEY, Lana Louise SMITH KEENAN, Roger John SNOW, Ronald John SORCEK, Hidenori TAKAHASHI, Steven John TAYLOR, Michael Robert TURNER, Erick Richard Roush YOUNG, Qiang ZHANG, Yunlong ZHANG, Renee M. ZINDELL
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Publication number: 20140005103Abstract: The present invention relates to Sulfonamide Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, W, X, R1, R2, R3, R4 and R5 are as defined herein. The present invention also relates to compositions comprising at least one Sulfonamide Derivative, and methods of using the Sulfonamide Derivatives for improving the pharmacokinetics of a drug.Type: ApplicationFiled: June 25, 2013Publication date: January 2, 2014Inventors: Craig A. Coburn, Milana Maletic, Richard Soll, Chunsing Li, Yunfu Luo, Zhiqi Qi
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Patent number: 8618110Abstract: The present invention includes and relates generally to compounds of structural Formula (I), or a salt, solvate, or prodrug thereof, which modulate apoptosis in cells. The present invention also provides pharmaceutical compositions containing these compounds, methods of making these compounds, and methods of using these compounds and pharmaceutical compositions for treatment of diseases associated with irregular apoptosis in cells.Type: GrantFiled: February 9, 2010Date of Patent: December 31, 2013Assignee: VM Discovery Inc.Inventors: Jay Jie-Qiang Wu, Ling Wang
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Publication number: 20130345200Abstract: Herein are disclosed indoles of formula (I) where the various groups are defined herein, and which are useful for treating cancer.Type: ApplicationFiled: August 7, 2013Publication date: December 26, 2013Applicant: GlaxoSmithKline LLCInventors: James Brackley, III, Joelle Lorraine Burgess, Seth Grant, Neil Johnson, Steven D. Knight, Louis Lafrance, William H. Miller, Kenneth Newlander, Stuart Romeril, Meagan B. Rouse, Xinrong Tian, Sharad Kumar Verma
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Publication number: 20130345228Abstract: The present invention relates to novel 3,4-dihydro-pyrrolo[1,2-a]pyrazin-1-ylamine derivatives as inhibitors of beta-secretase, also known as beta-site amyloid cleaving enzyme, BACE, BACE1, Asp2, or memapsin2. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which beta-secretase is involved, such as Alzheimer's disease (AD), mild cognitive impairment, senility, dementia, dementia with Lewy bodies, Down's syndrome, dementia associated with stroke, dementia associated with Parkinson's disease or dementia associated with beta-amyloid.Type: ApplicationFiled: March 7, 2012Publication date: December 26, 2013Applicant: JANSSEN PHARMACEUTICAL NVInventors: Andrés Avelino Trabanco-Suárez, Francisca Delgado-Jiménez
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Patent number: 8609659Abstract: Diazapolycyclic compounds having affinity for the opioidergic receptors, preferably for the delta opioidergic receptors, with central and/or peripheral activity, having formula: A1-D1-T1??(I) wherein: A1 is a group of formula (II): wherein: R1 is phenyl wherein one of the ring hydrogen atoms is substituted with a group selected from C(O)R?, C(O)OR?, C(O)NHR? or C(O)NR3R4, R?, R3 and R4, being as defined in the application; R2 is phenyl, optionally substituted D1 is a diazapolycyclic group T1 is a group selected from H, alkyl, alkenyl, alkynyl and from the following optionally substituted groups: cycloalkyl, heterocycloalkyl, aryl, heteroaryl, cycloalkylalkyl, heterocycloalkylalkyl, arylalkyl or heteroarylalkyl, and their hydrates and solvates and pharmaceutically acceptable salts.Type: GrantFiled: December 13, 2010Date of Patent: December 17, 2013Assignee: Neuroscienze Pharmaness S.C.A.R.L.Inventors: Paolo Lazzari, Giovanni Loriga, Stefania Ruiu, Gabriele Murineddu, Luca Pani, Gerard Aime Pinna
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Publication number: 20130331395Abstract: The present invention is directed to bridged aryl piperazine derivatives, pharmaceutical compositions containing them and their use in the treatment of depression and related disorders. The compounds of the present invention are serotonin transport inhibitors and/or modulators of 5HT1A.Type: ApplicationFiled: August 9, 2013Publication date: December 12, 2013Applicant: Janssen Pharmaceutica NVInventors: Christopher Creighton, Tina Morgan Ross, Allen B. Reitz, Cheryl P. Kordik, Steven Paget, Gregor J. Macdonald
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Patent number: 8604195Abstract: In its many embodiments, the present invention relates to a novel class of substituted bicyclic piperidinyl- and piperazinylsulfonamide compounds useful to inhibit 11?-hydroxysteroid dehydrogenase type-I, pharmaceutical compositions containing the compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the expression of 11?-hydroxysteroid dehydrogenase type-I using such compounds or pharmaceutical compositions.Type: GrantFiled: August 12, 2008Date of Patent: December 10, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Unmesh Shah, Craig D. Boyle, Samuel Chackalamannil
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Publication number: 20130317035Abstract: Certain quinolizidine and octahydropyridopyrazine compounds, pharmaceutical compositions, and methods of their use, inter alia, as opioid receptor antagonists are disclosed.Type: ApplicationFiled: July 25, 2013Publication date: November 28, 2013Applicant: Adolor CorporationInventors: Roland E. Dolle, Bertrand Le Bourdonnec, Allan James Goodman
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Publication number: 20130316408Abstract: The invention discloses marine Streptomyces sp., a Pyranosesquiterpene compound, as well as a preparation method and uses thereof. Streptomyces sp. SCSIO 01689 was collected in China Center for Type Culture Collection (CCTCC) (Address: Wuhan University, Wuhan City, China) with the collection number of CCTCC NO: M 2011257 on Jul. 18, 2011. The Streptomyces sp. SCSIO 01689 can produce the Pyranosesquiterpene compound with better anti-Escherichia coli activity and anti-Artemia activity, as well as Cyclo(D)-Pro-(D)-Ile, Cyclo(D)-Pro-(D)-Leu and Cyclo(D)-trans-4-OH-Pro-(D)-Phe with better anti-Vibrio anguillarum activity and anti-Artemia activity, thereby providing a new way for preparing the Cyclo(D)-Pro-(D)-Ile, the Cyclo(D)-Pro-(D)-Leu and the Cyclo(D)-trans-4-OH-Pro-(D)-Phe. The Pyranosesquiterpene compound can be used for preparing anti-Escherichia coli medicaments and anti-Artemia medicaments, as well as preparing condiments as a condiment precursor compound.Type: ApplicationFiled: June 18, 2012Publication date: November 28, 2013Applicant: South China Sea Institute Of Oceanology, Chinese Academy of SciencesInventors: Lijuan Long, Xinpeng Tian, Jie Li, Xiongming Luo, Zhenxiong Qi, Tuan Yin
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Patent number: 8580788Abstract: Certain quinolizidine and octahydropyridopyrazine compounds, pharmaceutical compositions, and methods of their use, inter alia, as opioid receptor antagonists are disclosed.Type: GrantFiled: May 24, 2012Date of Patent: November 12, 2013Assignee: Adolor CorporationInventors: Roland E. Dolle, Bertrand Le Bourdonnec, Allan James Goodman
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Publication number: 20130296564Abstract: Herein we describe compositions and methods for the synthesis of [2.2.2]-diazabicyclic structures comprising a domino reaction sequence involving aldol condensation, alkene isomerization, and intramolecular hetero-Diels-Alder cycloaddition. Excellent diastereofacial control during the cycloaddition is enforced with a removable chiral phenyl aminal diketopiperazine substituent. The reaction sequence rapidly generates molecular complexity and is competent with both enolizable and non-enolizable aldehyde substrates. This method provides an efficient route to [2.2.2]-diazabicyclic structures, common to bioactive prenylated indole alkaloids such as the brevianamides and stephacidins.Type: ApplicationFiled: May 1, 2013Publication date: November 7, 2013Applicant: College of William and MaryInventor: Jonathan R. Scheerer
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Publication number: 20130289232Abstract: To provide a novel cyclic amine compound and a process for producing a polyurethane resin by using it. A 3-hydroxy-1,5-diazabicyclo[3.2.2]nonane represented by the following formula (1), and a process for producing a polyurethane resin by using a catalyst for producing a polyurethane resin, which contains the 3-hydroxy-1,5-diazabicyclo[3.2.2]nonane. When the compound represented by the formula (1) has optical isomers, diastereomers or geometric isomers, the compound includes both a mixture of any of them and an isolated isomer of any of them. [in the above formula (1), each of R1, R2, R3, R4, R5, R6, R7 and R8 which are independent of one another, is a hydrogen atom, a C1-4 alkyl group, a hydroxy group, a hydroxymethyl group or a C1-4 alkoxy group.Type: ApplicationFiled: December 22, 2011Publication date: October 31, 2013Applicant: Tosoh CorporationInventors: Hiroyuki Kiso, Takao Suzuki, Yoshihiro Takahashi
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Patent number: 8569493Abstract: A method for preventing or treating a metabolic disorder, an inflammatory disease, an autoimmune disease, an allergic disease, a central nervous system disease, a cardiovascular disease, a homeostasis-related disease or glaucoma, involving administering a compound or a salt thereof, the compound having the following formula (1): wherein R1 represents alkyl, cycloalkyl, aryl, heterocyclic or aralkyl; R7 represents cycloalkyl, aryl or heterocyclic; W represents oxygen or NR8, Y represents alkylene, Z represents oxygen, sulfur, OCO or NR9; R2, R3, R4, R6, R8 and R9 represent hydrogen or alkyl.Type: GrantFiled: February 2, 2012Date of Patent: October 29, 2013Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Mamoru Matsuda, Toshiyuki Mori, Masato Nagatsuka, Sachiko Kobayashi, Masatomo Kato, Miwa Takai
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Patent number: 8569303Abstract: This invention is directed to compounds of formula (I): where r, q, R, R2, R3, R4, R5a, R5b, R5c, R6a, R6b, R6c, R7, R8, and R9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.Type: GrantFiled: April 30, 2010Date of Patent: October 29, 2013Assignee: Celtaxsys, Inc.Inventors: Damian O Arnaiz, Greg Brown, Emmanuel Claret, Arwed Cleve, David Davey, William Guilford, Seock-Kyu Khim, Thomas Kirkland, Monica J Kochanny, Amy Liang, David Light, John Parkinson, David Vogel, Guo Ping Wei, Bin Ye