Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To A Piperidine Ring Patents (Class 546/189)
  • Patent number: 10323009
    Abstract: The present disclosure provides pharmaceutical compositions comprising Gamma-glutamyl cycle inhibitors (GGCI) and certain pharmaceutically acceptable salts thereof, and methods of use.
    Type: Grant
    Filed: April 24, 2017
    Date of Patent: June 18, 2019
    Assignee: CANCER RESEARCH TECHOLOGY, LLP
    Inventors: David Rubin, Eyal Rubin
  • Publication number: 20150148543
    Abstract: The invention features methods and compositions for the synthesis of multimerizing agents.
    Type: Application
    Filed: January 28, 2015
    Publication date: May 28, 2015
    Inventors: Feng Li, Yihan Wang
  • Patent number: 9024028
    Abstract: The invention features methods and compositions for the synthesis of multimerizing agents. An exemplary method for producing AP20187 may comprise: (a) coupling 2-N,Ndimethylaminomethyl-1,3-diaminopropane with AP20792 to produce the dimeric alcohol, AP20793; and (b) coupling the AP20793 so produced with API7362 to yield AP20187. In particular embodiments, the method further includes the step of producing API7362 by coupling API7360 with methyl-L-pipecolic acid, or a salt thereof.
    Type: Grant
    Filed: January 26, 2012
    Date of Patent: May 5, 2015
    Assignee: ARIAD Pharmaceuticals, Inc.
    Inventors: Feng Li, Yihan Wang
  • Patent number: 9018200
    Abstract: Substituted piperidinyl compounds of the formula (I): are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.
    Type: Grant
    Filed: October 18, 2012
    Date of Patent: April 28, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Milana Maletic, Harold B. Wood, Wanying Sun
  • Publication number: 20150087628
    Abstract: K-Ras is the most frequently mutated oncogene in human cancer. Disclosed herein are compositions and methods for modulating K-Ras and treating cancer.
    Type: Application
    Filed: April 10, 2013
    Publication date: March 26, 2015
    Inventors: Jonathan Ostrem, Ulf Peters, Kevan M. Shokat
  • Patent number: 8981094
    Abstract: The invention relates to a DGAT inhibitor of formula (I): including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents —C(?O)—; —O—C(?O)—; C(?O)—C(?O)—; —NRx—C(?O)—; —Z1—C(O)—; —Z1—NRx—C(?O)—; —C(?O)—Z1—; —NRx—C(?O)—Z1—; —S(?O)p-; —C(?S)—; —NRx—C(?S)—; —Z1—C(?S)—; —Z1—NRx—C(?S)—; —C(?S)—Z1-; —NRx—C(?S)—Z—; Y represents NRx—C(=0)-Z2—; —NRx—C(=0)-Z2—NRy—; —NRx—C(=0)-Z2—NRy—C(=0)-; —NRx—C(=0)-Z2—NRy—C(=0)-O—; —NRx—C(=0)-Z2-0-; —NRx—C(=0)-Z2-0-C(=0)-; —NRx—C(=0)-Z2—C(=0)-; —NRx—C(=0)-Z2—C(=0)-; —NRx—C(=0)-0-Z2—C(=0)-; —NRx—C(=0)-0-Z2—C(=0)-0-; —NRx—C(?O)—O—Z2—O—C(?O)—; —NRx—C(?O)—Z2—C(?O)—NRy—; —NRx—C(?O)—Z2—NRy—C(=0)-NRy—; —C(?O)—Z2—; —C(?O)—Z2—O—; —C(=0)-NRx—Z2—; —C(=0)-NRx—Z2-0-; —C(=0)-NRx—Z2—C(=0)-0-; —C(=0)-NRx—Z2-0-C(=0)-; —C(=0)-NRx—Z2—NRy—; —C(=0)-NRx—Z2—NRy—C(=0)-; —C(=0)-NRx—Z2—NRy—C(=0)-0-; R1 represents C1-12alkyl optionally substituted with cyano, C1-4alkyloxy, C1-4alkyl-oxyC1-4alkylox
    Type: Grant
    Filed: June 6, 2008
    Date of Patent: March 17, 2015
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Jean-Pierre André Marc Bongartz, Joannes Theodorus Maria Linders, Lieven Meerpoel, Guy Rosalia Eugeen Van Lommen, Erwin Coesemans, Mirielle Braeken, Christophe Francis Robert Nestor Buyck, Monique Jenny Marie Berwaer, Katharina Antonia Germania J. M. De Waepenaert, Peter Walter Maria Roevens, Gustaaf Maria Boeckx, Petr Vladimirivich Davidenko
  • Publication number: 20140343075
    Abstract: The present invention relates to piperidine and pyrazine derivatives according to formulae (Ia), (Ib) and (II) as autotaxin inhibitors and the use of such compounds for the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by increased lysophosphatic acid levels and/or the activation of autotaxin, in particular of different cancers.
    Type: Application
    Filed: July 30, 2014
    Publication date: November 20, 2014
    Applicant: MERCK PATENT GMBH
    Inventors: Kai SCHIEMANN, Melanie SCHULTZ, Wolfgang STAEHLE
  • Publication number: 20140336193
    Abstract: The present invention relates to compounds that exhibit vasodilatory and anti-inflammatory effects by inhibiting the activity of soluble epoxide hydrolase (sEH). The present invention is also directed to methods of identifying such compounds, and use of such compounds for the treatment of diseases related to dysfunction of vasodilation, inflammation, and/or endothelial cells. In particular non-limiting embodiments, components of the invention may be used to treat hypertension.
    Type: Application
    Filed: July 23, 2014
    Publication date: November 13, 2014
    Inventors: Donald W. Landry, Shi-Xian Deng, Stevan Pecic, Kirsten Alison Rinderspacher
  • Publication number: 20140329803
    Abstract: This invention relates to compounds that are agonists of the muscarinic M1 receptor and which are useful in the treatment of muscarinic M1 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula I, where n is 1 or 2; p is 0, 1 or 2; q is 0, 1 or 2; and R1-R6 are as defined herein.
    Type: Application
    Filed: November 16, 2012
    Publication date: November 6, 2014
    Inventors: Miles Congreve, Giles Brown, Julie Cansfield, Benjamin Tehan
  • Publication number: 20140314669
    Abstract: The present invention relates to novel fluorine containing compounds, methods for their preparation, the intermediates of the synthesis, their use as diagnostic agents, especially for imaging of thrombi. The invention relates to positron emission tomography (PET) agents and associated precursor reagents, and methods for producing such radiolaveled agents for imaging of thrombi in a mammalian body. More particularly, the invention relates to small nonpeptide, high-affinity, specific-binding glycoprotein 11b/IIIa antagonists for imaging of thrombi.
    Type: Application
    Filed: August 17, 2012
    Publication date: October 23, 2014
    Applicant: PIRAMAL IMAGING SA
    Inventors: Markus Berger, Martin Kruger, Jessica Lohrke, Michael Reinhardt, Holger Siebeneicher
  • Patent number: 8859814
    Abstract: Disclosed is a compound of formula (I). Wherein R1, R2Ar and Cy are as defined herein, or a pharmaceutically acceptable salt thereof. Also disclosed are pharmaceutical compositions of the compound of formula (I), methods of making the compounds of formula I, and methods of using the compounds of formula (I) to treat a disorder associated with activation of CCR10.
    Type: Grant
    Filed: May 14, 2009
    Date of Patent: October 14, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Derek Cogan, Alexander Heim-Riether, Wang Mao, Craig Andrew Miller, Philip Dean Ramsden, Lana Louise Smith Keenan, Roger John Snow, Jiang-Ping Wu, Yu Yang
  • Publication number: 20140296202
    Abstract: Substituted piperidinyl compounds of the formula (I): are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.
    Type: Application
    Filed: October 18, 2012
    Publication date: October 2, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Milana Maletic, Harold B. Wood, Wanying Sun
  • Publication number: 20140256699
    Abstract: Substituted cyclopropyl compounds of the formula I and the pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the g-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included. Another aspect of the invention that is of interest relates to compounds of formula Ia.
    Type: Application
    Filed: September 24, 2012
    Publication date: September 11, 2014
    Inventors: Michael W. Miller, Andrew W. Stamford, Kallol Basu, Scott Edmondson, Zhiqiang Guo, William B. Geiss
  • Publication number: 20140187546
    Abstract: Cystine analogs that improve the solubility of L-cystine in urine for treatment of cystinuria and which have the structure: and pharmaceutically acceptable salts, solvates and prodrugs thereof, wherein each R and R? pair are independently selected from (i) or (ii); (i) R and R? are independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alcohol, substituted or unsubstituted aryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocyclic, and substituted or unsubstituted heteroaryl, or (ii) R and R? together form a substituted or unsubstituted heterocyclic ring structure, or a substituted or unsubstituted heteroaryl ring structure; X is hydrogen, or an alkyl; and Y is O or S.
    Type: Application
    Filed: January 2, 2014
    Publication date: July 3, 2014
    Applicant: Rutgers, The State University of New Jersey
    Inventors: Longqin Hu, Amrik Sahota
  • Publication number: 20140171649
    Abstract: The invention features methods and compositions for the synthesis of multimerizing agents. An exemplary method for producing AP20187 may comprise: (a) coupling 2-N,Ndimethylaminomethyl-1,3-diaminopropane with AP20792 to produce the dimeric alcohol, AP20793; and (b) coupling the AP20793 so produced with API7362 to yield AP20187. In particular embodiments, the method further includes the step of producing API7362 by coupling API7360 with methyl-L-pipecolic acid, or a salt thereof.
    Type: Application
    Filed: January 26, 2012
    Publication date: June 19, 2014
    Applicant: ARIAD PHARMACEUTICALS, INC.
    Inventors: Feng Li, Yihan Wang
  • Publication number: 20140154775
    Abstract: There are provided, inter alia, photolabile compounds and methods useful for the formation of dimers of biological molecules and subsequent dissociation of the dimers.
    Type: Application
    Filed: November 19, 2013
    Publication date: June 5, 2014
    Applicant: City of Hope
    Inventors: John C. Williams, David Horne, Jun Xie, Shubbir Ahmed
  • Patent number: 8691846
    Abstract: The present invention relates to piperidine sulphonamide derivatives of formula wherein Ar1, Ar2, R1, R2, m and n are as defined in the description and claims, or pharmaceutically suitable acid addition salts thereof. The compounds of formula I are orexin receptor antagonists and the related compounds can be useful in the treatment of sleep apnea, narcolepsy, insomnia, parasomnia, jet lag syndrome, circadian rhythms disorder or sleep disorders associated with neurological diseases.
    Type: Grant
    Filed: April 2, 2013
    Date of Patent: April 8, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Henner Knust, Matthias Nettekoven, Emmanuel Pinard, Olivier Roche, Mark Rogers-Evans
  • Publication number: 20140073573
    Abstract: The invention provides compounds that are effective as inhibitors of human plasmin and plasma kallikrein, and that are useful for the prevention of blood loss and as components of fibrin adhesives. The invention further provides methods of making and using the compounds.
    Type: Application
    Filed: October 31, 2013
    Publication date: March 13, 2014
    Applicant: THE MEDICINES COMPANY (LEIPZIG) GMBH
    Inventors: Peter HEROLD, Mohammed DAGHISH, Stjepan JELAKOVIC, Friedrich-Alexander LUDWIG, Claudia REICHELT, Alexander SCHULZE, Andrea SCHWEINITZ
  • Patent number: 8658131
    Abstract: Bipiperidinyl compounds and salts thereof are disclosed. The compounds include high affinity ligands for ?1 receptors. Some compounds are also highly selective for ?1 receptor compared to ?2 receptor. Compounds can comprise radioisotopes, including 18F or 11C. Radiolabeled compounds can be used as probes for imaging distribution of ?1 receptor in a subject such as a human using positron emission tomography (PET) scanning.
    Type: Grant
    Filed: June 21, 2011
    Date of Patent: February 25, 2014
    Assignee: Washington University
    Inventors: Zhude Tu, Robert H. Mach, Wei Wang, Stanley M. Parsons
  • Patent number: 8648094
    Abstract: Disclosed herein is an isomer, enantiomer, diastereoisomer or tautomer of a compound represented by Formula I: or a prodrug, or a pharmaceutically acceptable salt, or labeled with a detectable label or an affinity tag thereof; wherein R1, R1a, R100, R100a, R2, R200, W, B, and W1 are defined herein. Also disclosed are methods of using compounds of Formula I to treat proliferative disorders such as cancer.
    Type: Grant
    Filed: March 21, 2012
    Date of Patent: February 11, 2014
    Assignee: Pharmascience, Inc.
    Inventors: Alain Laurent, Scott Jarvis, Patrick Bureau, Alain Boudreault, James Jaquith
  • Publication number: 20140011996
    Abstract: Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted T-type calcium channel activity are disclosed. Specifically, a series of compounds containing N-piperidinyl acetamide derivatives as shown in formula (1).
    Type: Application
    Filed: August 29, 2013
    Publication date: January 9, 2014
    Applicant: Zalicus Pharmaceuticals Ltd.
    Inventors: Hassan Pajouhesh, Ramesh Kaul, Yanbing Ding, Yongbao Zhu, Lingyun Zhang, Nagasree Chakka, MIchael Edward Grimwood, Jason Tan, Yuanxi Zhou
  • Publication number: 20130324556
    Abstract: A compound of formula (I) or a pharmaceutically acceptable salt, solvate, or hydrate thereof Wherein Y, Z, R3, U, R4, m and n are as defined in the claims.
    Type: Application
    Filed: January 27, 2012
    Publication date: December 5, 2013
    Inventors: Joe William Boyd, Paul Meo, Michael Higginbottom, Iain Simpson, David Mark Mountford, Edward Daniel Savory
  • Publication number: 20130274475
    Abstract: Substituted bicyclic beta-lactams of Formula I: are ?-lactamase inhibitors, wherein a, X, R1 and R2 are defined herein. The compounds and pharmaceutically acceptable salts thereof are useful in the treatment of bacterial infections in combination with ?-lactam antibiotics. In particular, the compounds can be employed with a ?-lactam antibiotics (e.g., imipenem, piperacillin, or ceftazidime) against microorganisms resistant to ?-lactam antibiotics due to the presence of the ?-lactamases.
    Type: Application
    Filed: June 6, 2013
    Publication date: October 17, 2013
    Inventors: Ian MANGION, Nelo Rivera, Rebecca T. Ruck, Michael Shelvin
  • Patent number: 8541451
    Abstract: The invention provides two crystalline freebase forms of biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]methylamino}ethyl)piperidin-4-yl ester. The invention also provides pharmaceutical compositions comprising the crystalline freebase or prepared using the crystalline freebases; processes and intermediates for preparing the crystalline freebases; and methods of using the crystalline freebases to treat a pulmonary disorder.
    Type: Grant
    Filed: July 14, 2010
    Date of Patent: September 24, 2013
    Assignee: Theravance, Inc.
    Inventor: Grahame Woollam
  • Publication number: 20130217729
    Abstract: The present invention relates to piperidine sulphonamide derivatives of formula wherein Ar1, Ar2, R1, R2, m and n are as defined in the description and claims, or pharmaceutically suitable acid addition salts thereof. The compounds of formula I are orexin receptor antagonists and the related compounds can be useful in the treatment of sleep apnea, narcolepsy, insomnia, parasomnia, jet lag syndrome, circadian rhythms disorder or sleep disorders associated with neurological diseases.
    Type: Application
    Filed: April 2, 2013
    Publication date: August 22, 2013
    Inventors: Henner Knust, Matthias Nettekoven, Emmanuel Pinard, Olivier Roche, Mark Rogers-Evans
  • Publication number: 20130210827
    Abstract: 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: Application
    Filed: February 4, 2013
    Publication date: August 15, 2013
    Applicant: ABBVIE INC.
    Inventor: AbbVie Inc.
  • Patent number: 8481726
    Abstract: The present invention relates to a novel process for the preparation of specific sterically hindered nitroxyl ethers from their corresponding sterically hindered nitroxyl radicals by reacting it with an aldehyde and a hydroperoxide. This nitroxyl ether formation may be carried out from different starting nitroxyl radicals, which are subsequently further reacted to the desired compounds. The compounds prepared by this process are effective as stabilizers for polymers against harmful effects of light, oxygen and/or heat and as flame-retardants for polymers.
    Type: Grant
    Filed: June 25, 2007
    Date of Patent: July 9, 2013
    Assignee: BASF SE
    Inventors: Abdel-Ilah Basbas, Davide Alvisi, Robert Cordova, Michael Peter Difazio, Walter Fischer, Joseph A. Kotrola, Tiziano Nocentini, James Robbins, Kai-Uwe Schöning
  • Publication number: 20130165438
    Abstract: The present invention provides a piperidine compound represented by Formula (I) (wherein X1, X2, X2, A, B and N are as defined in the Description); or a salt thereof.
    Type: Application
    Filed: September 6, 2011
    Publication date: June 27, 2013
    Applicant: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Yoshihiro Urade, Makoto Kitade, Keiko Yamane, Shinichi Aoki, Hiroyoshi Yamanaka
  • Patent number: 8471031
    Abstract: The present invention relates to a novel process for the preparation of a sterically hindered nitroxyl ether from the corresponding sterically hindered nitroxyl radical by reacting it with a carbonyl compound and a hydroperoxide. The compounds prepared by this process are effective stabilizers for polymers against harmful effects of light, oxygen and/or heat, as flame-retardants for polymers and as polymerization regulators.
    Type: Grant
    Filed: June 25, 2007
    Date of Patent: June 25, 2013
    Assignee: BASF SE
    Inventors: Kai-Uwe Schöning, Walter Fischer, Abdel-Ilah Basbas, Alexander Dichtl
  • Patent number: 8455521
    Abstract: Diaminoalkanes of below Formula I have now been found which are orally active and bind to aspartic proteases to inhibit their activity: They are useful in the treatment or amelioration of diseases associated with elevated levels of aspartic protease activity. The invention also relates to a method for the use of the compounds of Formula I in ameliorating or treating aspartic protease related disorders in a subject in need thereof comprising administering to said subject an effective amount of a compound of Formula I.
    Type: Grant
    Filed: May 28, 2010
    Date of Patent: June 4, 2013
    Assignee: Vitae Pharmaceuticals, Inc.
    Inventors: John J. Baldwin, David A. Claremon, Colin M. Tice, Salvacion Cacatian, Lawrence W. Dillard, Alexey V. Ishchenko, Jing Yuan, Zhenrong Xu, Gerard McGeehan, Wei Zhao, Robert D. Simpson, Suresh B. Singh, Patrick T. Flaherty, Jean-Pierre Wery
  • Publication number: 20130129625
    Abstract: The present invention relates to the field of medical imaging, and in particular to imaging of disease states associated with the upregulation of the chemokine receptor 5 (CCR5). Imaging agents, precursors and methods are provided which are useful in imaging such disease states.
    Type: Application
    Filed: December 18, 2012
    Publication date: May 23, 2013
    Applicants: HAMMERSMITH IMANET LIMITED, GE HEALTHCARE LIMITED
    Inventors: GE Healthcare Limited, Hammersmith Imanet Limited
  • Patent number: 8436183
    Abstract: New compounds are disclosed for multimerizing immunophilins and proteins containing immunophilin or immunophilin-related domains. The compounds are of the formula M-L-Q where M is a synthetic ligand for an FKBP protein.
    Type: Grant
    Filed: January 30, 2012
    Date of Patent: May 7, 2013
    Assignee: ARIAD Pharmaceuticals, Inc.
    Inventors: Dennis A. Holt, Terence P. Keenan, Tao Guo, Edgardo Laborde, Wu Yang
  • Patent number: 8399485
    Abstract: Bipiperidyl compounds of the formula: (I) are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts and solvates are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.
    Type: Grant
    Filed: December 10, 2007
    Date of Patent: March 19, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Harold B. Wood, Alan D. Adams, Stanley Freeman, Jason W. Szewczyk, Conrad Santini, Yong Huang, Ralph T. Mosley
  • Publication number: 20130053385
    Abstract: The use of a compound of formula I wherein the substituents are as defined in claim 1, or compositions containing them in controlling insects, acarines, nematodes or molluscs.
    Type: Application
    Filed: December 7, 2010
    Publication date: February 28, 2013
    Applicants: SYNGENTA LIMITED, SYNGENTA CROP PROTECTION LLC
    Inventors: Stephane Andre Marie Jeanmart, Russell Viner, John Benjamin Taylor, William Guy Whittingham, Jeffrey Steven Wailes, Sarah Margaret Targett, Christopher John Mathews, Michel Muehlebach
  • Publication number: 20130045977
    Abstract: The present invention provides a compound represented by the following formula (I) or a physiologically acceptable salt thereof, and use thereof for the prophylaxis or treatment of TGF-?-related diseases: wherein Y is a hydrogen atom and the like; R2 is and the like; R3 is —NR8—R9— and the like; R4, R5, R6 and R7 are the same or different and each is a hydrogen atom and the like; and X is and the like.
    Type: Application
    Filed: February 17, 2011
    Publication date: February 21, 2013
    Applicant: KYOTO UNIVERSITY
    Inventors: Hideaki Kakeya, Akira Hattori, Yasuaki Takasu, Nobutaka Fujii, Shinya Oishi, Soichi Kojima, Mitsuko Hara
  • Publication number: 20130023563
    Abstract: Provided are a novel amidine derivative having an activated blood coagulation factor X inhibitory activity, a production method thereof, a production intermediate therefor, and a pharmaceutical composition containing the amidine derivative. An amidinoaniline derivative represented by the following formula (1-1) or a pharmaceutically acceptable salt thereof: <in the formula (1-1), each symbol is as defined in the Description>, and a pharmaceutical composition containing the amidinoaniline derivative or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: September 26, 2012
    Publication date: January 24, 2013
    Applicant: AJINOMOTO CO., INC.
    Inventor: AJINOMOTO CO., INC.
  • Publication number: 20130023660
    Abstract: Disclosed are carboxamide compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure in which R1, R2, R3, R4, D, J, Z, T, p, q, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.
    Type: Application
    Filed: September 18, 2012
    Publication date: January 24, 2013
    Applicant: RIGEL PHARMACEUTICALS, INC.
    Inventors: Jiaxin Yu, Hui Hong, Ihab S. Darwish, Xiang Xu, Rajinder Singh
  • Publication number: 20120302539
    Abstract: Certain compounds and pharmaceutically acceptable salts are provided herein. Also provided are pharmaceutical compositions comprising at least one compound or pharmaceutically acceptable salt therein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain disease states responsive to the inhibition of transglutaminase TG2 activity are described. These disease states include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound or pharmaceutically acceptable salt thereof as a single active agent or administering at least one compound or pharmaceutically acceptable salt thereof in combination with one or more other therapeutic agents.
    Type: Application
    Filed: May 7, 2012
    Publication date: November 29, 2012
    Inventors: Michael Prime, Stephen Martin Courtney, Richard Marston, Celia Dominguez, Douglas Macdonald, John Wityak
  • Patent number: 8288417
    Abstract: The present invention relates to inhibitors of 11-? hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-? hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.
    Type: Grant
    Filed: October 24, 2011
    Date of Patent: October 16, 2012
    Assignee: Incyte Corporation
    Inventors: Wenqing Yao, Meizhong Xu, Colin Zhang, Yanlong Li, Jincong Zhuo, Brian W. Metcalf
  • Patent number: 8273894
    Abstract: This invention provides compounds of formula I: wherein a, b, c, d, m, n, p, s, t, W, Ar1, R1, R2, R3, R4, R6, R7, and R8 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.
    Type: Grant
    Filed: April 3, 2012
    Date of Patent: September 25, 2012
    Assignee: Theravance, Inc.
    Inventors: Mathai Mammen, YuHua Ji, YongQi Mu, Craig Husfeld, Li Li
  • Publication number: 20120238602
    Abstract: The present invention relates to piperidine sulphonamide derivatives of formula wherein Ar1, Ar2, R1, R2, m and n are as defined in the description and claims, or pharmaceutically suitable acid addition salts thereof. The compounds of formula I are orexin receptor antagonists and the related compounds can be useful in the treatment of sleep apnea, narcolepsy, insomnia, parasomnia, jet lag syndrome, circadian rhythms disorder or sleep disorders associated with neurological diseases.
    Type: Application
    Filed: May 23, 2012
    Publication date: September 20, 2012
    Inventors: Henner Knust, Matthias Nettekoven, Emmanuel Pinard, Olivier Roche, Mark Rogers-Evans
  • Publication number: 20120237874
    Abstract: According to one embodiment, an actinic-ray- or radiation-sensitive resin composition includes any of the compounds (A) of general formula (I) below that when exposed to actinic rays or radiation, generates an acid and a resin (B) whose rate of dissolution into an alkali developer is increased by the action of an acid. (The characters used in general formula (I) have the meanings mentioned in the description.
    Type: Application
    Filed: May 31, 2012
    Publication date: September 20, 2012
    Applicant: FUJIFILM CORPORATION
    Inventors: Shuhei Yamaguchi, Akinori Shibuya
  • Patent number: 8262945
    Abstract: Photochromic compositions are disclosed comprising a polymeric material, a photochromic dye, a hydroxyphenyl triazine UV absorber and, optionally, a further light stabilizer selected from the sterically hindered amines. These systems provide a reversible photochromic effect and show improved light stabilization and color fastness.
    Type: Grant
    Filed: July 24, 2009
    Date of Patent: September 11, 2012
    Assignee: BASF SE
    Inventors: Mara Destro, Dario Lazzari, Dirk Simon, Manuele Vitali
  • Publication number: 20120220564
    Abstract: Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted T-type calcium channel activity are disclosed using a series of compounds containing N-acylated cyclic amines linked to an a?l ring as shown in formula (I).
    Type: Application
    Filed: September 17, 2010
    Publication date: August 30, 2012
    Applicant: Zalicus Pharmaceuticals Ltd.
    Inventors: Hassan Pajouhesh, Yongbao Zhu, Yuanxi Zhou, Michael E. Grimwood, Eric Simonson
  • Publication number: 20120183751
    Abstract: The present invention is to provide a photosensitive resin composition which has excellent resolution, is low in cost and is applicable to a wide range of applications due to the structure of a polymer precursor in which reaction into a final product is promoted by a basic substance or by heating in the presence of a basic substance. The present invention is also to provide a base generator which is applicable to such a photosensitive resin composition. Disclosed is a base generator which has a specific structure and generates a base by exposure to electromagnetic radiation and heating. Also disclosed is a photosensitive resin composition which comprises the base generator and a polymer precursor in which reaction into a final product is promoted by a basic substance or by heating in the presence of a basic substance.
    Type: Application
    Filed: September 29, 2010
    Publication date: July 19, 2012
    Applicant: DAI NIPPON PRINTING CO., LTD.
    Inventors: Mami Katayama, Shunji Fukuda, Katsuya Sakayori
  • Patent number: 8188090
    Abstract: The invention is concerned with the compounds of formula I: and pharmaceutically acceptable salts and esters thereof, wherein X, Q and R1-R3 are defined in the detailed description and claims. The invention is also concerned with the compounds of formula Z: and pharmaceutically acceptable salts and esters thereof, wherein R1-R3 are defined in the detailed description and claims. In addition, the present invention relates to methods of manufacturing and using the compounds of formula I and Z as well as pharmaceutical compositions containing such compounds. The compounds of formula I and Z are antagonists or partial agonists at the CRTH2 receptor and may be useful in treating diseases and disorders associated with that receptor such as asthma.
    Type: Grant
    Filed: November 9, 2009
    Date of Patent: May 29, 2012
    Assignee: Hoffman-La Roche Inc.
    Inventors: Fariborz Firooznia, Tai-An Lin, Sung-Sau So, Baoxia Wang, HongYing Yun
  • Publication number: 20120129837
    Abstract: Chemical agents, such as disulfonamide derivatives of fluorene, anthracene, xanthene, dibenzosuberone and acridine, and similar heterocyclic ring structures, including salts thereof, that act as anti-cancer and anti-tumor agents, especially where such agents modulate the activity of the Wnt/?-catenin signaling pathway, and serve to reduce ?-catenin levels present in cells, such as cancer cells, or where the agents modulate levels of gene expression in cellular systems, including cancer cells, are disclosed, along with methods for preparing such agents, as well as pharmaceutical compositions containing such agents as active ingredients and methods of using these as therapeutic agents.
    Type: Application
    Filed: January 30, 2012
    Publication date: May 24, 2012
    Inventors: Wieslaw M. Cholody, Yi Zang, Norman E. Ohler, Sheela Chellappan, Janak Padia, Karina Zuck, Jeffrey W.H. Watthey, Zoe Ohler, Jeffrey Strovel
  • Publication number: 20120130076
    Abstract: New compounds are disclosed for multimerizing immunophilins and proteins containing immunophilin or immunophilin-related domains. The compounds are of the formula M-L-Q where M is a synthetic ligand for an FKBP protein.
    Type: Application
    Filed: January 30, 2012
    Publication date: May 24, 2012
    Applicant: ARIAD Pharmaceuticals, Inc.
    Inventors: Dennis A. Holt, Terence P. Keenan, Tao Guo, Edgardo Laborde, Wu Yang
  • Publication number: 20120115907
    Abstract: The present invention relates to novel renin inhibitors of general formula (1), novel intermediates involved in their synthesis, their pharmaceutically acceptable salts and pharmaceutical compositions containing them. The present invention also relates to a process of preparing compounds of general formula (1), their tautomeric forms, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and novel intermediates involved in their synthesis.
    Type: Application
    Filed: April 22, 2010
    Publication date: May 10, 2012
    Applicant: CADILA HEALTHCARE LIMITED
    Inventors: Pravain Thombare, Jigar Desai, Mukul R. Jain
  • Publication number: 20120088791
    Abstract: In one aspect, the invention relates to compounds having a general structure: Formula (I) which are useful as allosteric agonists of the M1 muscarinic receptor, synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurodegenerative diseases, including Alzheimer's Disease. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: February 19, 2010
    Publication date: April 12, 2012
    Applicant: VANDERBILT UNIVERSITY
    Inventors: Craig W. Lindsley, Jeffrey P. Corn, Charles David Weaver, Colleen M. Niswender, Evan P. Lebois, Thomas M. Bridges