Acyclic Nitrogen Bonded Directly To A -c(=x)- Group, Wherein X Is Chalcogen Patents (Class 546/247)
  • Publication number: 20150141437
    Abstract: The use of compounds of formula wherein R2, R3, R4, R5, R6 and R7 have several meanings, for the treatment of disorders mediated by protozoan organisms, novel compounds of the above formula and intermediates for the preparation of such compounds, pharmaceutical compositions comprising such novel compounds, a method of treating disorders mediated by protozoan organisms comprising administering such compounds, optionally together with a second drug substance, to a subject in need thereof and the use of such compounds, whenever comprising a photoaffinity label, for the identification of the molecular target(s) of arylamino alcohol antimalarials.
    Type: Application
    Filed: June 10, 2013
    Publication date: May 21, 2015
    Inventors: Hubert Gstach, Peter Chiba, Matthias Mastalir
  • Publication number: 20150126516
    Abstract: A piperidine compound represented by the following Formula (1): wherein ring A, ring B, and ring C are the same or different and each represent a benzene ring or a nitrogen-containing heteroaromatic ring; W represents a C1-C4 alkylene or alkenylene group; X, Y, and Z are the same or different and each represent a halogen atom, a C1-C6 alkyl group, a halo C1-C6 alkyl group, a C1-C6 alkoxy group, or a halo C1-C6 alkoxy group; m, n, and p are the same or different and each represent an integer of 0 to 5; when m is greater than or equal to 2, the Xs are the same or different; when n is greater than or equal to 2, the Ys are the same or different; and when p is greater than or equal to 2, the Zs are the same or different has an excellent controlling efficacy against pests.
    Type: Application
    Filed: April 12, 2013
    Publication date: May 7, 2015
    Inventor: Sadayuki Arimori
  • Patent number: 9018381
    Abstract: The present invention relates to compounds of Formula (I): and to their salts, pharmaceutical compositions, methods of use, and methods for their preparation. These compounds inhibit Bcl-2 and/or Bcl-XL activities and may be used for the treatment of cancer.
    Type: Grant
    Filed: August 5, 2011
    Date of Patent: April 28, 2015
    Assignee: AstraZeneca AB
    Inventors: Robert Bruce Diebold, Thomas Gero, Paul Grover, Shan Huang, Stephanos Ioannidis, Claude Afona Ogoe, Jamal Carlos Saeh
  • Publication number: 20150065392
    Abstract: A reactive mass label for labelling a biological molecule for detection by mass spectrometry includes the following structure: X-L-M-S-Re, wherein X is a mass marker moiety, L is a cleavable linker, M is a mass normalization moiety, and S is a mass series modifying group including the following group: wherein J is C?O, K is NH, and n is 2 or J and K are both CH2 and n is 1, m is at least 1; and Re is a reactive functionality for attaching the reactive mass label to a biological molecule.
    Type: Application
    Filed: September 15, 2014
    Publication date: March 5, 2015
    Applicant: Electrophoretics Limited
    Inventors: Christian Baumann, Stefan Kienle, Karsten Kuhn, Harald Legner
  • Publication number: 20150025077
    Abstract: This invention relates to geranylgeranyl acetone (GGA) derivatives and the use of GGA, its isomers, and GGA derivatives in methods for inhibiting neural death, increasing neural activity, increasing axon growth and cell viability, and increasing the survival rate of subjects administered the GGA or GGA derivatives.
    Type: Application
    Filed: February 27, 2013
    Publication date: January 22, 2015
    Applicant: COYOTE PHARMACEUTICALS, INC.
    Inventors: Hiroaki Serizawa, Ankush B. Argade, Akash Datwani, Natalie Spencer, Yonghua Pan, Florian Ermini
  • Publication number: 20140336185
    Abstract: Compounds that bind the glucagon-like peptide 1 (GLP-1) receptor, methods of their synthesis, methods of their therapeutic and/or prophylactic use, and methods of their use in stabilizing GLP-1 receptor in vitro for crystallization of the GLP-1 receptor are provided. Certain compounds may have activity as modulators or potentiators with respect to glucagon receptor, GIP receptor, GLP-1 and GLP-2 receptors, and PTH receptor on their own or in the presence of receptor ligands such as GIP (1-42), PTH (1-34), Glucagon (1-29), GLP-2 (1-33), GLP-1 (7-36), GLP-1 (9-36), oxyntomodulin and exendin variants.
    Type: Application
    Filed: May 31, 2012
    Publication date: November 13, 2014
    Inventors: Marcus F. Boehm, Esther Martinborough, Manisha Moorjani, Junko Tamiya, Liming Huang, Thomas Fowler, Andrew Novak, Premji Meghani, Enugurthi Brahmachary, Adam Richard Yeager
  • Publication number: 20140294978
    Abstract: The present invention provides a cationic lipid and the like. The cationic lipid is for delivering a medicament containing a cationic lipid which facilitates the introduction of a nucleic acid into a cell or the like, and is represented by formula (I).
    Type: Application
    Filed: March 12, 2014
    Publication date: October 2, 2014
    Applicant: Kyowa Hakko Kirin Co., Ltd.
    Inventors: Takeshi KUBOYAMA, Kaori YAGI, Tomoyuki NAOI, Tomohiro ERA
  • Publication number: 20140187531
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic protein family members, compositions containing the compounds and uses of the compounds for preparing medicaments for treating diseases during which occurs expression one or more than one of an anti-apoptotic protein family member.
    Type: Application
    Filed: March 3, 2014
    Publication date: July 3, 2014
    Applicant: AbbVie Inc.
    Inventors: Milan Bruncko, Hong Ding, Steven W. Elmore, Aaron R. Kunzer, Christopher L. Lynch, William J. McClellan, Cheol-Min Park, Andrew M. Petros, Xiaohong Song, Xilu Wang, Noah P. Tu, Michael D. Wendt, Alexander R. Shoemaker, Michael J. Mitten
  • Publication number: 20140163017
    Abstract: In one aspect, the invention relates to substituted (E)-N?-(1-phenylethylidene)benzohydrazide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of lysine-specific histone demethylase, including LSD1; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the LSD1. 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: June 19, 2013
    Publication date: June 12, 2014
    Applicant: UNIVERSITY OF UTAH
    Inventors: Hariprasad Vankayalapati, Venkataswamy Sorna, Steven L. Warner, Bret Stephens, David J. Bearss, Sunil Sharma
  • Patent number: 8669252
    Abstract: Compounds of structural formula I are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to the enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders.
    Type: Grant
    Filed: May 12, 2011
    Date of Patent: March 11, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Dong-Ming Shen, John S. Debenham, Thomas H. Graham, Matthew J. Clements, Yong Zhang
  • Publication number: 20130296323
    Abstract: This invention relates to geranylgeranyl acetone (GGA) derivatives and the use of GGA, its isomers, and GGA derivatives in methods for inhibiting neural death, increasing neural activity, increasing axon growth and cell viability, and increasing the survival rate of subjects administered the GGA or GGA derivatives.
    Type: Application
    Filed: February 27, 2013
    Publication date: November 7, 2013
    Applicant: COYOTE PHARMACEUTICALS, INC.
    Inventors: Hiroaki Serizawa, Ankush B. Argade, Akash Datwani, Natalie Spencer, Yonghua Pan, Florian Ermini
  • Patent number: 8575350
    Abstract: Disclosed herein cost effective and ecofriendly large scale process for producing pyridine carboxylic acid with high purity and yield at industrial scale.
    Type: Grant
    Filed: September 12, 2011
    Date of Patent: November 5, 2013
    Assignee: Jubilant Life Sciences Ltd
    Inventors: Shailendra Kumar Singh, Neeraj Tiwari, Ashutosh Agarwal
  • Publication number: 20130190488
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic protein family members, compositions containing the compounds and uses of the compounds for preparing medicaments for treating diseases during which occurs expression one or more than one of an anti-apoptotic protein family member.
    Type: Application
    Filed: December 12, 2012
    Publication date: July 25, 2013
    Applicant: Abbott Laboratories
    Inventor: Abbott Laboratories
  • Patent number: 8486965
    Abstract: The present invention provides a fused heterocycle derivative having a strong Smo inhibitory activity, and use thereof. Specially, the present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or salt thereof, and a medicament containing the compound or a prodrug thereof, which is an Smo inhibitor or an agent for the prophylaxis or treatment of cancer.
    Type: Grant
    Filed: August 25, 2010
    Date of Patent: July 16, 2013
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Tomohiro Ohashi, Zenyu Shiokawa, Yuta Tanaka, Satoshi Sasaki
  • Publication number: 20130178494
    Abstract: The present disclosure relates to new DNA-directed alkylating agents and water-soluble N-mustard agents with improved chemical stability and anti-tumor therapeutic efficacy.
    Type: Application
    Filed: June 29, 2012
    Publication date: July 11, 2013
    Applicant: Academia Sinica
    Inventors: Tsann-Long SU, Ting-Chao Chou, Te-Chuang Lee
  • Patent number: 8461189
    Abstract: The present invention relates to a novel class of pyridyl and pyrimidinyl derivatives. The pyridyl and pyrimidinyl compounds can be used to treat cancer. The pyridyl and pyrimidinyl compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.
    Type: Grant
    Filed: June 24, 2008
    Date of Patent: June 11, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Richard W. Heidebrecht, Jr., Thomas A. Miller, Matthew G. Stanton, David J. Witter
  • Publication number: 20130143876
    Abstract: The invention relates to new piperidine derivatives of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    Type: Application
    Filed: December 3, 2012
    Publication date: June 6, 2013
    Inventors: Gerald Juergen ROTH, Martin FLECK, Thorsten LEHMANN-LINTZ, Bernd NOSSE
  • Patent number: 8389553
    Abstract: The present invention relates to a novel class of 4-carboxybenzylamino derivatives. The 4-carboxybenzylamino compounds can be used to treat cancer. The 4-carboxybenzylamino compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.
    Type: Grant
    Filed: June 24, 2008
    Date of Patent: March 5, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Paul Harrington, Solomon Kattar, Thomas A. Miller, Matthew G. Stanton, Paul Tempest, David J. Witter
  • Patent number: 8377968
    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: Grant
    Filed: April 8, 2009
    Date of Patent: February 19, 2013
    Assignee: Zalicus Pharmaceuticals, Ltd.
    Inventors: Hassan Pajouhesh, Ramesh Kaul, Yanbing Ding, Yongbao Zhu, Lingyun Zhang, Nagasree Chakka, Mike Grimwood, Jason Tan, Yuanxi Zhou
  • Publication number: 20130035351
    Abstract: The present invention relates to non-charged oxime compounds which are acetyl cholinesterase (AChE) reactivators of inhibited AChE and which protect against organophosphate poisoning both peripherally and in the central nervous system. Also disclosed are pharmaceutical compositions and methods for preparing the reactivator compounds and associated intermediates.
    Type: Application
    Filed: August 3, 2011
    Publication date: February 7, 2013
    Applicant: SOUTHWEST RESEARCH INSTITUTE
    Inventors: Stanton F. MCHARDY, Richard M. CORBETT, Donald M. MAXWELL, Michael W. TIDWELL, Bismarck CAMPOS, Christopher J. BEMBEN
  • Publication number: 20120283137
    Abstract: A reactive mass label for labelling a biological molecule for detection by mass spectrometry, which label comprises a reactive functionality for labelling thiol groups or carbonyl groups. Also provided is a reactive mass label for labelling a biological molecule for detection by mass spectrometry, wherein the mass label comprises the following structure: X-L-M-S-Re wherein X is a mass marker moiety, L is a cleavable linker, M is a mass normalization moiety, S is a mass series modifying group comprising the following group: wherein J is C?O, K is NH, and n is 2 or J and K are both CH2 and n is 1, and wherein m is at least 1; and Re is a reactive functionality for attaching the mass label to a biological molecule.
    Type: Application
    Filed: September 8, 2010
    Publication date: November 8, 2012
    Applicant: ELECTROPHORETICS LIMITED
    Inventors: Christian Baumann, Stefan Kienle, Karsten Kuhn, Harald Legner
  • Publication number: 20120136073
    Abstract: There are provided for herein novel amine-containing transfection compounds and methods for making and using same. The compounds are generally obtained by reacting a primary amine with an unsaturated compound. Transfection complexes made using the amine-containing transfection compounds in combination with additional compounds to encapsulate biologically active agents such as nucleic acids are also provided for herein. Methods of using the transfection complexes for the in vivo or in vitro delivery of biologically active agents are also described. The transfection complexes of the present invention are highly potent, thereby allowing effective modulation of a biological activity at relatively low doses compared to analogous transfection compounds known in the art.
    Type: Application
    Filed: November 15, 2011
    Publication date: May 31, 2012
    Applicant: LIFE TECHNOLOGIES CORPORATION
    Inventors: Zhiwei Yang, Parul Angrish, Xavier de Mollerat du Jeu, Kristin Wiederholt
  • Patent number: 8188289
    Abstract: Inhibitors of the soluble epoxide hydrolase (sEH) are provided that incorporate multiple pharmacophores and are useful in the treatment of diseases.
    Type: Grant
    Filed: March 13, 2007
    Date of Patent: May 29, 2012
    Assignee: The Regents of the University of California
    Inventors: Bruce D. Hammock, Paul D. Jones, Christophe Morisseau, Huazhang Huang, Hsing-Ju Tsai, Richard Gless
  • Publication number: 20120095042
    Abstract: Provided are compounds of formula (I) wherein m is 0, 1 or 2; RI is a mono- or bicyclic heterocyclic ring system including one, two or three heteroatoms selected from nitrogen, sulphur and oxygen; R2 is selected from hydrogen, methyl and ethyl; I) R3 is hydrogen, methyl, or ethyl; and R4 and R5 are independently selected from ethyl and isopropyl; and R3, R4 and R5 together have at least 6 carbon atoms: or II) any two or all of R3, R4 and R5 form together with the carbon atom to which they are attached 3-para-menthyl, bornyl, or adamantyl; having cooling properties, their use as cooling agent and compositions including them.
    Type: Application
    Filed: May 4, 2010
    Publication date: April 19, 2012
    Inventor: Stefan Michael Furrer
  • Patent number: 8129358
    Abstract: Disclosed are new substituted pyrazole and triazole compounds of Formula (I) and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the derivatives together with pharmaceutically acceptable carriers, and uses thereof:
    Type: Grant
    Filed: November 8, 2007
    Date of Patent: March 6, 2012
    Assignee: Novartis AG
    Inventors: Yi Xia, Kris G. Mendenhall, Paul A. Barsanti, Annette O. Walter, David Duhl, Paul A. Renhowe
  • Publication number: 20120035134
    Abstract: The present invention relates to compounds of Formula (I): and to their salts, pharmaceutical compositions, methods of use, and methods for their preparation. These compounds inhibit Bcl-2 and/or Bcl-XL activities and may be used for the treatment of cancer.
    Type: Application
    Filed: August 5, 2011
    Publication date: February 9, 2012
    Applicant: ASTRAZENECA AB
    Inventors: Robert Bruce DIEBOLD, Thomas GERO, Paul GROVER, Shan HUANG, Stephanos IOANNIDIS, Claude Afona OGOE, Jamal Carlos SAEH, Jeffrey Gilbert VARNES
  • Publication number: 20120029021
    Abstract: Nitroxide free radicals attached to antineoplastic agents can synergize their potencies to cancer cells. This invention relates to any antineoplastic agents and their derivatives chemically attached with nitroxide free radicals, such as TEMPO and its radical derivatives. This invention also relates to precursors of such compounds, as well as the products formed from the adducts after administration.
    Type: Application
    Filed: January 17, 2011
    Publication date: February 2, 2012
    Applicant: THE TRUSTEES OF CALIFORNIA STATE UNIVERSITY
    Inventors: Yong Ba, Errol V. Mathias
  • Publication number: 20110275615
    Abstract: An amide of the formula I and its tautomeric forms, possible enantiomeric and diastereomeric forms, E and Z forms, and possible physiologically tolerated salts, in which the variables have the following meanings: A —(CH2)p—R1, where R1 can be pyrrolidine, morpholine, piperidine, —NR5R6 and and R5, R6 and R7 can, independently of one another, be hydrogen, C1-C4-alkyl, CH2Ph, Ph, CH2CH2Ph, it also being possible for the phenyl rings to be substituted by R6, and p can be 1 and 2, and B can be phenyl, pyridyl, pyrimidyl and pyridazyl, it also being possible for the rings to be substituted by up to 2 R8 radicals, and D can be a bond, —(CH2)m—, —CH?CH—, —C?C—, and R2 is chlorine, bromine, fluorine, C1-C6-alkyl, NHCO—C1-C4-alkyl, NHSO2—C1-C4-alkyl, NO2, —O—C1-C4-alkyl and NH2, and R3 is —C1-C6-alkyl, branched or unbranched, and which may also carry a phenyl ring, indolyl ring or cyclohexyl ring which is in turn substituted by a maximum of two R8 radicals, where R8 is hydrogen, C1-C4-alkyl, branched or un
    Type: Application
    Filed: October 29, 2010
    Publication date: November 10, 2011
    Inventors: Hans-Jörg Treiber, Monika Knopp, Wilfried Lubisch, Achim Moeller
  • Patent number: 8039471
    Abstract: The present invention provides a compound of Formula I or Formula II: enantiomer, diastereomer, prodrug, solvate, metabolite, or pharmaceutically acceptable salt thereof, wherein constituent variables are provided herein. The compounds of Formula I and II are modulators of metalloproteases and are useful in treating diseases associated with metalloprotease activity such as arthritis, cancer, cardiovascular disorders, skin disorders, inflammation and allergic conditions.
    Type: Grant
    Filed: December 3, 2008
    Date of Patent: October 18, 2011
    Assignee: Incyte Corporation
    Inventors: Wenqing Yao, Jincong Zhuo, Meizhong Xu, Fenglei Zhang, Brian Metcalf
  • Publication number: 20110224213
    Abstract: The invention relates to the use of glutaric acid derivatives of general formula (I), which are disclosed in the invention description, as anti-arrhythmic agents.
    Type: Application
    Filed: March 18, 2009
    Publication date: September 15, 2011
    Inventors: Vladimir Evgenievich Nebolsin, Dmitry Sergeevich Blinov, Vladimir Pavlovich Balashov, Tatyana Alexandrovna Kromova, Galina Alexandrovna Zheltukhina
  • Publication number: 20110212997
    Abstract: This invention relates to novel piperidine-4-acetamide derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
    Type: Application
    Filed: August 25, 2009
    Publication date: September 1, 2011
    Applicant: NEUROSEARCH A/S
    Inventors: Dan Peters, John Paul Redrobe, Elsebet Ostergaard Nielsen
  • Publication number: 20110207739
    Abstract: A series of novel 1,2-disubstituted amido-anthraquinone derivatives, and the preparation method and application of said derivatives. Said application includes said derivatives with therapeutically effective amount being prepared into pharmaceutical compositions for inhibition of cancer cell growth, further treating cancer.
    Type: Application
    Filed: February 25, 2010
    Publication date: August 25, 2011
    Inventor: Hsu-Shan HUANG
  • Patent number: 7951821
    Abstract: This invention discloses and claims a compound of general formula (I) in which R1 represents either a hydrogen atom, or an optionally substituted alkyl group, or a cycloalkylalkyl group, or an optionally substituted phenylalkyl group, or an alkenyl group, X represents a hydrogen atom or one or more substituents chosen from halogen atoms and trifluoromethyl, alkyl and alkoxy groups, R2 represents one or more substituents chosen from halogen atoms, optionally substituted alkoxy and optionally substituted amino. The compounds of this invention exhibit therapeutic utility.
    Type: Grant
    Filed: March 1, 2007
    Date of Patent: May 31, 2011
    Assignee: sanofi-aventis
    Inventors: Gihad Dargazanli, Genevieve Estenne-Bouhtou, Benoit Marabout, Pierre Roger, Mireille Sevrin
  • Publication number: 20110105488
    Abstract: The present application relates to pyrrolidine, piperidine, and other nitrogen-containing heterocyclic derivatives and the use of these compounds for treating and preventing pam or inflammation. The analgesic compounds demonstrate efficacy in the treatment of neuropathic pain resulting from a variety of conditions such as diabetic neuropathy, HIV infections, and post-herpetic neuralgia.
    Type: Application
    Filed: March 20, 2009
    Publication date: May 5, 2011
    Applicant: Chlorion Pharma, Inc.
    Inventors: Giorgio Attardo, Sasmita Tripathy
  • Patent number: 7919626
    Abstract: The invention provides a compound of formula I: wherein R1-R6, X, Y, and B have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of MAO-B enzyme function and are useful for improving cognitive function and for treating psychiatric disorders in animals.
    Type: Grant
    Filed: February 27, 2007
    Date of Patent: April 5, 2011
    Assignee: Helicon Therapeutics, Inc.
    Inventors: Xianbo Zhou, Roderick E. M. Scott, Rusiko Bourtchouladze, Alan P. Kaplan, Terence P. Keenan, Andrew McRiner
  • Publication number: 20110071125
    Abstract: This invention relates to novel substituted phenylamino-benzene compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: May 9, 2008
    Publication date: March 24, 2011
    Inventors: Joachim Rudolph, Jaques Dumas, Li Yingfu, Daniel Auclair, Mario Lobell, Marion Hitchcock, Ingo Hartung, Marcus Koppitz, Dominic Brittain, Florian Puehler, Kirstin Petersen, Judith Guenther, Benjamin Bader
  • Patent number: 7902181
    Abstract: The present invention provides compounds of formula (I) in which n, y, X1, X2, A, B, R1, R2, R3, R4 and R5 are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Grant
    Filed: December 10, 2008
    Date of Patent: March 8, 2011
    Assignee: AstraZeneca AB
    Inventors: Mark Furber, Christopher Andrew Luckhurst, Hitesh Jayantilal Sanganee, Linda Anne Stein, Peter Alan Cage
  • Patent number: 7893093
    Abstract: The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.
    Type: Grant
    Filed: March 22, 2006
    Date of Patent: February 22, 2011
    Assignee: ViroBay, Inc.
    Inventor: Craig J. Mossman
  • Publication number: 20110039802
    Abstract: The present invention provides a pharmaceutical composition for use as an NPY Y5 receptor antagonist comprising a compound of the formula (I): wherein R1 is lower alkyl, cycloalkyl or the like, R2 is hydrogen, lower alkyl or the like, n is 1 or 2, X is lower alkylone, lower alkenylene, arylene, cycloalkylene or the like, Y is CONR7, CSNR7, NR7CO, NR7CS or the like, Z is lower alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl or the like and R7 is hydrogen or lower alkyl, prodrug, pharmaceutically acceptable salt or solvate thereof
    Type: Application
    Filed: July 2, 2010
    Publication date: February 17, 2011
    Inventors: Yasuyuki KAWANISHI, Hideyuki TAKENAKA, Kohji HANASAKI, Tetsuo OKADA
  • Publication number: 20110015230
    Abstract: This present disclosure relates to novel compounds, isomer thereof or pharmaceutically acceptable salts thereof as vanilloid receptor (Vanilloid Receptor 1; VR1; TRPV1) antagonist; and a pharmaceutical composition containing the same. The present disclosure provides a pharmaceutical composition for preventing or treating a disease such as pain, migraine, arthralgia, neuralgia, neuropathies, nerve injury, skin disorder, urinary bladder hypersensitiveness, irritable bowel syndrome, fecal urgency, a respiratory disorder, irritation of skin, eye or mucous membrane, stomach-duodenal ulcer, inflammatory diseases, ear disease, heart disease and so on.
    Type: Application
    Filed: January 28, 2009
    Publication date: January 20, 2011
    Applicant: Amorepacific Corporation
    Inventors: Song Seok Shin, Jin Kwan Kim, Sun-Young Kim, Ki-Wha Lee, Byoung young Woo, Joo-Hyun Moh, Yeon Su Jeong, Kyung Min Lim, Jin Kyu Choi, Hyun-Ju Koh, Young-Ho Park
  • Publication number: 20100324049
    Abstract: [Problems] To provide an antagonist of a melanin-concentrating hormone receptor, which is useful as a medicine for a central nervous system disease, a cardiovascular disease or a metabolic disease. [Means for Solving Problems] The antagonist comprises, as an active ingredient, a compound represented by the formula (I) wherein R1a and R1b independently represent a hydrogen atom or a C1-6 alkyl group; R2a, R2b, R3a and R3b independently represent a hydrogen atom, a C1-6 alkyl group, or the like; Y represents H or —OH; Z represents —OR8, or the like; R8 represents a hydrogen atom, a C1-6 alkyl group which may have a substituent, or the like; R9a and R9b independently represent a hydrogen atom, a C1-6 alkyl group, or the like; Ar1 represents an aromatic carbon ring group, or an aromatic heteroring group; Ar2 represents a group produced by removing two hydrogen atoms from an aromatic carbon ring, or the like; and the ring group A represents an unsaturated heteroring group.
    Type: Application
    Filed: September 26, 2008
    Publication date: December 23, 2010
    Inventors: Makoto Ando, Minoru Kameda, Hiroshi Miyazoe, Minoru Moriya, Etsuko Hirose, Takao Suzuki
  • Publication number: 20100324046
    Abstract: The present invention relates to a novel class of 4-carboxybenzylamino derivatives. The 4-carboxybenzylamino compounds can be used to treat cancer. The 4-carboxybenzylamino compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.
    Type: Application
    Filed: June 24, 2008
    Publication date: December 23, 2010
    Inventors: Paul Harrington, Richard W. Heidebrecht, JR., Solomon Kattar, Thomas A. Miller, Karin M. Otte, Phieng Siliphaivanh, Paul Tempest, Kevin J. Wilson, David J. Witter
  • Publication number: 20100298278
    Abstract: The invention relates to the substituted 1,2-ethylenediamines of general formula (I), wherein the groups R1 to R13, A, B, L and i are defined as in the description and the claims. The invention also relates to the use thereof in the treatment of Alzheimer's disease (AD) and similar diseases.
    Type: Application
    Filed: August 8, 2006
    Publication date: November 25, 2010
    Inventors: Christian Eickmeier, Klaus Fuchs, Niklas Heine, Stefan Peters, Cornelia Dorner-Ciossek, Sandra Handschuh, Herbert Nar, Klaus Klinder
  • Publication number: 20100292467
    Abstract: Disclosed is a chemical compound having the structure: wherein R1 is an all group, aryl group, alkylaryl group or arylalkyl group with at least 23 carbon atoms, R2 is an alkylene group, arylene group, alkyarylene group or arylalkylene group with at least 2 carbons and X is a quaternary ammonium salt.
    Type: Application
    Filed: May 18, 2009
    Publication date: November 18, 2010
    Applicant: XEROX CORPORATION
    Inventors: Adela GOREDEMA, Aaron STRONG, Peter ODELL, C. Geoffrey ALLEN, Mihaela Maria BIRAU
  • Publication number: 20100292229
    Abstract: The present invention concerns compounds and their use to treat cell proliferative diseases such as cancer. In general aspects, compounds of the present invention are tyrphostin-like in structure. Compounds of the present invention, in certain embodiments, display significant potency by causing, for example, inhibition of Stat3 activation, reduction in c-myc protein levels and/or induction of apoptosis in tumor cells. In general aspects, compounds of the present invention induce one or more of these activities at nanomolar concentrations and typically function through a unique mechanism involving the induction of stress granules that bind specific signaling molecules and prevent them from participating in signal transduction and oncogenesis.
    Type: Application
    Filed: July 2, 2007
    Publication date: November 18, 2010
    Applicant: The Board of Regents of the University of Texas System
    Inventors: Nicholas J Donato, David Maxwell, Moshe Talpaz, William Bornmann, Zhenghong PENG, Ashutosh Pal, Dongmei Han, Shimei Wang, Geoffrey Bartholomeusz, Vaibhav Kapuria
  • Publication number: 20100286162
    Abstract: HPV inhibitors of formula (I) in which G1 is —NHCO(CH2)n-, where n is an integer between 1 and 4, R3 is —CW(CH2)m—NR4R5 or —CW(CH2)mCH3 or —CN, where W is O, S or NH and m is an integer between 0 and 5, or R3 is one of the following groups: and A is an optionally substituted aryl group and B is an aryl group, preferably a phenyl which is substituted.
    Type: Application
    Filed: November 20, 2008
    Publication date: November 11, 2010
    Inventors: Marta Blumenfeld, Delphine Compere, Jean-Michel Gauthier
  • Patent number: 7812100
    Abstract: The invention relates to new alkoxyamines suitable for hydrosilylation reactions, to siloxane modified alkoxamines and to siloxane modified polymers as well as to their use. The alkoxamines are compounds of formula (I) or (II) wherein A is a group capable of forming a stable free nitroxyl radical A. which is bound via its oxygen atom to the carbon atom; R.sub.1 and R.sub.2 independently of one another are hydrogen, C.sub.1-C.sub.18-alkyl, C.sub.3-C.sub.8cycloalkyl or phenyl which are unsubstituted or substituted by NO.sub.2, halogen, amino, hydroxy, cyano, carboxy, C.sub.1-C.sub.4alkoxy, C.sub.1-C.sub.4alkylthio, C.sub.1-C.sub.4alkylamino or di(C.sub.1-C.sub.4alkyl)amino; R.sub.3, R.sub.4 and R.sub.5 independently of one another are hydrogen or C.sub.1-C.sub.18alkyl or phenyl; or R.sub.3 and R.sub.5 together with the linking group C.dbd.C form a 5 to 12 membered ring; R.sub.6 is X hydrogen or C.sub.1-C.sub.l8alkyl or phenyl; X is O, NH or NR.sub.7, wherein R.sub.7 is C.sub.1-C.sub.18alkyl, C.sub.3-C.sub.
    Type: Grant
    Filed: October 16, 2006
    Date of Patent: October 12, 2010
    Assignee: Ciba Corporation
    Inventors: Lothar Alexander Engelbrecht, Peter Nesvadba
  • Publication number: 20100234427
    Abstract: This invention relates to novel 1-phenethylpiperidine derivatives useful as opioid receptor ligands. More specifically, the invention provides compounds useful as ? opioid receptor ligands. In other aspects the invention relates to the use of these compounds in a method for therapy, such as for the treatment of pain, and to pharmaceutical compositions comprising the compounds of the invention.
    Type: Application
    Filed: February 13, 2007
    Publication date: September 16, 2010
    Inventors: Dan Peters, Birgitte L. Eriksen, Gordon Munro, Elsebet Østergaard Nielsen, John Paul Redrobe
  • Publication number: 20100216841
    Abstract: The present invention is directed to 4-fluoro-piperidine compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which T-type calcium channels are involved. 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 T-type calcium channels are involved.
    Type: Application
    Filed: June 28, 2006
    Publication date: August 26, 2010
    Inventors: James C. Barrow, Craig W. Lindsley, William D. Shipe, Zhiqiang Yang, David Wisnoski
  • Patent number: 7781459
    Abstract: The invention relates to acyl-carboxyphenylurea derivatives and to their physiologically tolerated salts and physiologically functional derivatives. Compounds of the formula I, in which the radicals have the stated meanings, and the physiological tolerated salts thereof and processes for preparing them are described. The compounds are suitable for example for the treatment of type II diabetes.
    Type: Grant
    Filed: December 20, 2006
    Date of Patent: August 24, 2010
    Assignee: Sanofi-Aventis Deutschland GmbH
    Inventors: Elisabeth DeFossa, Dieter Kadereit, Thomas Klabunde, Hans-Joerg Burger, Andreas Herling, Karl-Ulrich Wendt, Erich Von Roedern, Karl Schoenafinger, Alfons Enhsen