Additional Hetero Ring Containing Patents (Class 546/268.1)
  • Publication number: 20140088071
    Abstract: Compounds of Formula (IA) and Formula (IB) are described. They are useful as stimulators of sGC, particularly NO-independent, heme-dependent stimulators. These compounds may be useful for treating, preventing or managing various disorders that are herein disclosed.
    Type: Application
    Filed: November 2, 2011
    Publication date: March 27, 2014
    Applicant: Ironwood Pharmaceuticals, Inc.
    Inventors: Takashi Nakai, Thomas Wai-Ho Lee, Charles Kim, Joel Moore, Nicholas Robert Perl, Jason Rohde
  • Publication number: 20140080803
    Abstract: Disclosed herein are modulators of TRPV3 of Formula (I) wherein p is 1, 2, 3, or 4, and G1, X1, X2, X3, X4, X5, G2, Z1, Ra, Rb, and u are as defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also presented.
    Type: Application
    Filed: October 23, 2012
    Publication date: March 20, 2014
    Applicant: AbbVie Inc.
    Inventors: Erol K. Bayburt, Bruce Clapham, Phil B. Cox, Jerome F. Daanen, Michael J. Dart, Gregory A. Gfesser, Arthur Gomtsyan, Michael E. Kort, Philip R. Kym, Robert G. Schmidt, Eric A. Voight
  • Patent number: 8674138
    Abstract: The present invention relates to a new binaphthalene derivative, a preparation method thereof, and an organic electronic device using the same. The binaphthalene derivative according to the present invention can perform functions of hole injection and transportation, electron injection and transportation, or light emission in an organic electronic device including an organic light-emitting device, and the device according to the present invention has excellent characteristics in terms of efficiency, drive voltage and stability, and in particular excellent effects such as a low voltage and a long life time.
    Type: Grant
    Filed: October 20, 2006
    Date of Patent: March 18, 2014
    Assignee: LG Chem. Ltd.
    Inventors: Jae Soon Bae, Dae Woong Lee, Dong Hoon Lee, Jae Chol Lee, Jun Gi Jang
  • Publication number: 20140073796
    Abstract: The present invention discloses a nitropyridinyl ethyleneimine compound as shown in the formula I and a preparation method of the same, as well as use of the compound in manufacture of a prodrug and in manufacture of a drug for treating a tumor.
    Type: Application
    Filed: November 14, 2013
    Publication date: March 13, 2014
    Applicant: Beijing Yiling Bioengineering Co., Ltd
    Inventors: Shangjin Yang, Jianhui Yan, Ligang Wang, Xingna Guo, Shubin Li, Guoqiang Wu, Ruiya Zuo, Xin Huang, Hongtao Wang, Lingling Wang, Wenjuan Huang, Huigang Lu, Ke Feng, Fang Li, Huimin He, Yu Liu
  • Patent number: 8669255
    Abstract: 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: Grant
    Filed: September 26, 2012
    Date of Patent: March 11, 2014
    Assignee: AbbVie Inc.
    Inventors: Tao Li, Sachin V. Patel, Richard J. Perner, John T. Randolph, Michael R. Schrimpf, Kevin R. Woller, Zhiren Xia, Qingwei Zhang
  • Publication number: 20140066421
    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: May 17, 2012
    Publication date: March 6, 2014
    Applicant: SOUTHWEST RESEARCH INSTITUTE
    Inventors: Stanton F. McHardy, Richard M. Corbett, Donald M. Maxwell, Michael W. Tidwell, Bismarck Campos, Christopher J. Bemben
  • Publication number: 20140066420
    Abstract: The present invention relates to wherein each symbol is as defined in the specification. The compound of the present invention has a superior RBP4-lowering action, and is useful as a medicament for the prophylaxis or treatment of disease and condition mediated by increased RBP4.
    Type: Application
    Filed: October 16, 2013
    Publication date: March 6, 2014
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Shizuo KASAI, Tomohiro KAKU, Masahiro KAMAURA
  • Patent number: 8664401
    Abstract: The present invention is directed to a new class of hydroxamic acid derivatives of formula I, wherein the variables G, T, D, L, R1, R2, R3 are as described herein, their use as LpxC inhibitors, and more specifically their use to treat bacterial infections in a patient in need thereof.
    Type: Grant
    Filed: December 6, 2010
    Date of Patent: March 4, 2014
    Assignee: Pfizer Inc.
    Inventors: Matthew Frank Brown, Ye Che, Anthony Marfat, Michael Joseph Melnick, Justin Ian Montgomery, Usa Reilly
  • Patent number: 8658661
    Abstract: The present invention relates to compound of formula (I): or pharmaceutically acceptable salts thereof, wherein R1-R5 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Grant
    Filed: August 12, 2011
    Date of Patent: February 25, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Alessandra Bartolozzi, Todd Bosanac, Zhidong Chen, Stephane De Lombaert, John D. Huber, Ho Yin Lo, Pui Leng Loke, Weimin Liu, Tina Marie Morwick, Alan Olague, Doris Riether, Heather Tye, Lifen Wu, Renee M. Zindell
  • Publication number: 20140051680
    Abstract: This invention relates to generally inhibiting histone deacetylase (HDAC) enzymes (e.g., HDAC1, HDAC2, and HDAC3).
    Type: Application
    Filed: February 28, 2012
    Publication date: February 20, 2014
    Applicant: REPLIGEN CORPORATION
    Inventors: Vincent Jacques, James R. Rusche, Norton P. Peet, Jasbir Singh
  • Patent number: 8653062
    Abstract: The present invention relates to novel cyclic amine and cycloalkyl derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Grant
    Filed: November 22, 2010
    Date of Patent: February 18, 2014
    Assignee: Allergan, Inc.
    Inventors: Phong X. Nguyen, Todd M. Heidelbaugh
  • Patent number: 8648074
    Abstract: 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: Grant
    Filed: September 26, 2012
    Date of Patent: February 11, 2014
    Assignee: AbbVie Inc.
    Inventors: Tao Li, Sachin V. Patel, Richard J. Perner, John T. Randolph, Michael R. Schrimpf, Kevin R. Woller, Zhiren Xia, Qingwei Zhang
  • Patent number: 8642774
    Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, X, R1, R2, R3 have meanings given in the description.
    Type: Grant
    Filed: December 3, 2012
    Date of Patent: February 4, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Matthias Grauert, Daniel Bischoff, Georg Dahmann, Raimund Kuelzer, Klaus Rudolf, Bernd Wellenzohn
  • Publication number: 20140031331
    Abstract: The present invention relates to aminotetraline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminotetraline derivatives, and the use of such aminotetraline derivatives for therapeutic purposes. The aminotetraline derivatives are GlyT1 inhibitors.
    Type: Application
    Filed: September 19, 2013
    Publication date: January 30, 2014
    Inventors: Wilhelm Amberg, Michael Ochse, Udo Lange, Andreas Kling, Berthold Behl, Wilfried Hornberger, Mario Mezler, Charles W. Hutchins
  • Patent number: 8633213
    Abstract: Crystalline forms of imatinib mesylate (F, G, H, I and K) and their respective characterization are disclosed.
    Type: Grant
    Filed: May 15, 2012
    Date of Patent: January 21, 2014
    Assignee: Novartis AG
    Inventor: Michael Mutz
  • Patent number: 8633222
    Abstract: Novel vinylazacycloalkane compounds of Formula (I) are disclosed. The compounds are ligands of various nAChRs. The compounds and their pharmaceutically acceptable salts can be used to prepare pharmaceutical compositions and/or medicaments intended to prevent or treat disorders associated with dysfunction of nAChRs, especially within the central nervous system or the gastrointestinal system. Examples of types of disorders that can be treated include neurodegenerative disorders, including central nervous system disorders such as Alzheimer's disease, cognitive disorders, motor disorders such as Parkinson's disease, drug addiction, behavioral disorders and inflammatory disorders within the gastrointestinal system. The compounds can also serve as analgesics in the treatment of acute, chronic or recurrent pain.
    Type: Grant
    Filed: February 24, 2011
    Date of Patent: January 21, 2014
    Assignee: Targacept, Inc.
    Inventors: Jeffrey Daniel Schmitt, Gary Maurice Dull, Arielle Genevois-Borella, Marc Capet, Michel Cheve, Craig Harrison Miller
  • Patent number: 8629165
    Abstract: Disclosed herein are methods of treating a patient suffering a cognitive disorder.
    Type: Grant
    Filed: April 5, 2012
    Date of Patent: January 14, 2014
    Assignees: Allergan, Inc., Exonhit Therapeutics SA
    Inventors: John E. Donello, Fabien J. Schweighoffer, Lauren M. Luhrs
  • Patent number: 8623860
    Abstract: The invention relates to new azetidine derivatives of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    Type: Grant
    Filed: December 14, 2012
    Date of Patent: January 7, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Martin Fleck, Bernd Nosse, Gerald Juergen Roth
  • Patent number: 8618305
    Abstract: The present invention provides dimethyl sulphoxide solvate of 4-(4-{3-[4-chloro-3 -(trifluoromethyl)phenyl]ureido}phenoxy)-N2-methylpyridine-2-carboxamide, process for its preparation, pharmaceutical composition comprising it and its use for the treatment of cancer. The present invention also provides a novel HPLC method for the identification, quantification and isolation of related substances of sorafenib.
    Type: Grant
    Filed: January 28, 2011
    Date of Patent: December 31, 2013
    Assignee: Ranbaxy Laboratories Limited
    Inventors: Jagdev Singh Jaryal, Swargam Sathyanarayana, Rajesh Kumar Thaper, Mohan Prasad, Sachin Deorao Zade, Ajay Shankar Singh
  • Patent number: 8618304
    Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, R20 to R22 and R50 have the meanings indicated in the claims, which are pharmaceutically active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: May 1, 2012
    Date of Patent: December 31, 2013
    Assignee: Sanofi
    Inventors: Josef Pernerstorfer, Heinz-Werner Kleemann, Matthias Schaefer, Alena Safarova, Marcel Patek
  • Patent number: 8614329
    Abstract: The present invention provides amorphous and crystalline forms of acid addition salts of sorafenib, pharmaceutical compositions comprising them, and their use for the treatment of cancer. The present invention also provides processes for the preparation of acid addition salts of sorafenib.
    Type: Grant
    Filed: June 7, 2013
    Date of Patent: December 24, 2013
    Assignee: Ranbaxy Laboratories Limited
    Inventors: Jagdev Singh Jaryal, Swargam Sathyanarayana, Rajesh Kumar Thaper, Mohan Prasad
  • Patent number: 8614215
    Abstract: The present invention is related to quinoxaline compounds of Formula (I) in particular for the treatment of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.
    Type: Grant
    Filed: February 21, 2008
    Date of Patent: December 24, 2013
    Assignee: Merck Serono SA
    Inventors: Pascale Gaillard, Vincent Pomel, Isabelle Jeanclaude-Etter, Jerome Dorbais, Jasna Klicic, Cyril Montagne
  • Patent number: 8609851
    Abstract: The present invention discloses a nitropyridinyl ethyleneimine compound as shown in the formula I and a preparation method of the same, as well as use of the compound in manufacture of a prodrug and in manufacture of a drug for treating a tumor.
    Type: Grant
    Filed: October 27, 2009
    Date of Patent: December 17, 2013
    Assignee: Beijing Yiling Bioengineering Co., Ltd.
    Inventors: Shangjin Yang, Jianhui Yan, Ligang Wang, Xingna Guo, Shubin Li, Guoqiang Wu, Ruiya Zuo, Xin Huang, Hongtao Wang, Lingling Wang, Wenjuan Huang, Huigang Lu, Ke Feng, Fang Li, Huimin He, Yu Liu
  • Patent number: 8609705
    Abstract: Disclosed is a harmful arthropod control composition comprising, as an active ingredient, a fused heterocyclic compound represented by formula (1) [wherein A1 and A2 independently represent a nitrogen atom or the like; R1 and R4 independently represent a halogen atom or the like; R2 and R3 independently represent a halogen atom or the like; R5 and R6 independently represent a linear C1-C6 hydrocarbon group which may be substituted, or the like (provided that both R5 and R6 cannot represent a hydrogen atom simultaneously); and n represents 0 or 1]. The harmful arthropod control composition has an excellent efficacy to control harmful arthropods.
    Type: Grant
    Filed: March 8, 2013
    Date of Patent: December 17, 2013
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Mitsuhiko Iwakoshi, Ippei Uemura
  • Patent number: 8604034
    Abstract: The present invention relates to compounds of formula (I) its salts, isomers or prodrugs thereof useful in the treatment of viral infections, in particular respiratory syncytial virus (RSV) infections. The present invention also relates to processes for preparing the compounds and intermediates used in their preparation.
    Type: Grant
    Filed: February 8, 2011
    Date of Patent: December 10, 2013
    Assignee: Biota Scientific Management Pty Ltd.
    Inventors: Jeffrey Peter Mitchell, Gary Pitt, Alistair George Draffan, Penelope Anne Mayes, Laura Andrau, Kelly Anderson
  • Patent number: 8604208
    Abstract: The present invention provides amorphous and crystalline forms of acid addition salts of sorafenib, pharmaceutical compositions comprising them and their use for the treatment of cancer. The present invention also provides processes for the preparation of acid addition salts of sorafenib.
    Type: Grant
    Filed: September 24, 2010
    Date of Patent: December 10, 2013
    Assignee: Ranbaxy Laboratories Limited
    Inventors: Jagdev Singh Jaryal, Swargam Sathyanarayana, Rajesh Kumar Thaper, Mohan Prasad
  • Patent number: 8598209
    Abstract: The subject invention relates to novel P2X3 receptor antagonists that play a critical role in treating disease states associated with pain, in particular peripheral pain, inflammatory pain, or tissue injury pain that can be treated using a P2X3 receptor subunit modulator.
    Type: Grant
    Filed: October 21, 2009
    Date of Patent: December 3, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christopher S. Burgey, Zhengwu J. Deng, Diem N. Nguyen, Daniel V. Paone, Anthony W. Shaw, Anthony Ginnetti
  • Patent number: 8592440
    Abstract: Crystalline forms of imatinib mesylate (F, G, H, I and K) and their respective characterizations are disclosed.
    Type: Grant
    Filed: July 15, 2011
    Date of Patent: November 26, 2013
    Assignee: Novartis AG
    Inventor: Michael Mutz
  • Patent number: 8586571
    Abstract: The present invention relates to wherein each symbol is as defined in the specification. The compound of the present invention has a superior RBP4-lowering action, and is useful as a medicament for the prophylaxis or treatment of disease and condition mediated by increased RBP4.
    Type: Grant
    Filed: October 17, 2008
    Date of Patent: November 19, 2013
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Shizuo Kasai, Tomohiro Kaku, Masahiro Kamaura
  • Patent number: 8586740
    Abstract: Provided is a compound represented by the following formula (G21). Further, provided is a light-emitting element including a layer including a compound represented by the following formula (G21) between a pair of electrodes. In the formula (G21), two pyridine skeletons are respectively bonded to 2-position and 3-position of a quinoxaline skeleton arylene groups.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: November 19, 2013
    Assignee: Semiconductor Energy Laboratory Co., Ltd.
    Inventors: Hiroshi Kadoma, Sachiko Kawakami, Satoko Shitagaki, Satoshi Seo
  • Publication number: 20130303506
    Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
    Type: Application
    Filed: July 22, 2013
    Publication date: November 14, 2013
    Applicant: Janssen Pharmaceutical N.V.
    Inventors: Patrick René Angibaud, Kristof Van Emelen, Virginie Sophie Poncelet, Bruno Roux
  • Patent number: 8580799
    Abstract: The present invention relates to hydroximoyl-heterocycle derivatives of formula (I) wherein T represents a substituted or non-substituted heterocyclyl group, Q represents a carbo or heterocyclic group, A represent a carbo or heterocyclic group or a carbo or hetero-polycylic group, and L1 represents various linking groups, their process of preparation, intermediate compounds for their preparation, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.
    Type: Grant
    Filed: December 8, 2009
    Date of Patent: November 12, 2013
    Assignee: Bayer Cropscience AG
    Inventors: Christian Beier, Jurgen Benting, David Bernier, Pierre-Yves Coqueron, Philippe Desbordes, Christophe Dubost, Stephanie Gary, Pierre Genix, Daniela Portz, Ulrike Wachendorff-Neumann
  • Patent number: 8575351
    Abstract: Disclosed herein is an active metabolite (“M20”) of a molecule that is useful as a thrombin receptor antagonist: Also disclosed are formulations of this compound, synthetic routes to this compound, and methods of treating a variety of cardiovascular conditions, including acute coronary syndrome and peripheral arterial disease, and of effecting secondary prevention, by orally administering the active metabolilte.
    Type: Grant
    Filed: June 2, 2010
    Date of Patent: November 5, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Kimberly Nguyen Voronin, Natalia A. Penner
  • Patent number: 8569331
    Abstract: The present invention relates to substituted benzo[f]imidazo[1,2-d]pyrido[2,3-b][1,4]diazepine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted benzo[f]imidazo[1,2-d]pyrido[2,3-b][1,4]diazepine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.
    Type: Grant
    Filed: November 1, 2011
    Date of Patent: October 29, 2013
    Assignee: ArQule, Inc.
    Inventors: Mark A. Ashwell, Sudharshan Eathiraj, Anton Filikov, Steffi Koerner, Jean-Marc Lapierre, Yanbin Liu, Rocio Palma, David Vensel, Shin Iimura, Akiko Shiina, Kenichi Yoshida, Takanori Yamazaki, Akihisa Matsuda
  • Patent number: 8557999
    Abstract: Anatabine citrate and formulations containing anatabine citrate are useful for promoting health and well-being.
    Type: Grant
    Filed: May 22, 2012
    Date of Patent: October 15, 2013
    Assignee: Rock Creek Pharmaceuticals, Inc.
    Inventors: Tom Thomas Puthiaparampil, Thomas Kanathkunn David, Muppala Sarveswara Raju
  • Patent number: 8552197
    Abstract: The present invention provides sorafenib ethane sulphonate, process for its preparation, pharmaceutical composition comprising sorafenib ethane sulphonate and its use for the treatment of cancer. Formula (III).
    Type: Grant
    Filed: November 12, 2010
    Date of Patent: October 8, 2013
    Assignee: Ranbaxy Laboratories Limited
    Inventors: Jagdev Singh Jaryal, Swargam Sathyanarayana, Rajesh Kumar Thaper, Mohan Prasad
  • Patent number: 8551426
    Abstract: Provided are an RNase activity inhibitory compound to effectively control the activity of the RNase promoting degradation of extracted RNAs and, in addition, a sample storage container including the same. The RNase activity inhibitory compound and the sample storage container according to the present invention may be effectively used to store RNAs during RNA extraction or the extracted RNAs.
    Type: Grant
    Filed: June 12, 2009
    Date of Patent: October 8, 2013
    Assignee: Bioneer Corporation
    Inventors: Jong Hoon Kim, Hwangseo Park, Han Oh Park
  • Publication number: 20130261100
    Abstract: The invention relates pyridine amide derivative of Formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are independently hydrogen, linear o branched (C1-C3)alkyl or joined together they form a cyclopropyl ring; R is independently selected from the group consisting of halogens and trifluoromethyl and p is 1, 2 or 3; A is C or N; E is a group of formula (B) or (C), wherein B is C(O)OH, C(O)O(C1-C3)alkyl, and C is selected from the group consisting of formula (I) m is 1,2 or 3, n is 0 or 1, W is —O—, —O(C1-C3 alkyl)-; —(C1-C3 alkyl)O—; —C(O)—; —C(?N—O(C1-C3 alkyl))-; —NH— or —NH(C1-C3alkyl)-; Ar is phenyl, optionally substituted with one or more substituents selected from the group consisting of halogen, trifluoromethyl, trifluoromethoxy, methyl, —NH(C1-C3alkyl)-; —N(C1-C3alkyl)(C1-C3alkyl)-, a from 5 to 7 membered heterocyclic ring containing one nitrogen atom which is covalently bonded to Ar and optionally containing one or two heteroatoms selected from N, O and S; and a 5- or 6-member
    Type: Application
    Filed: December 10, 2010
    Publication date: October 3, 2013
    Inventors: Manuela Borriello, Lucio Rovati, Luigi Piero Stasi, Benedetta Buzzi, Fabrizio Colace
  • Patent number: 8541450
    Abstract: The invention relates to enantiomerically pure 3-(phthalimido)piperidines and processes for preparing enantiomerically pure 3-(phthalimido)piperidines.
    Type: Grant
    Filed: March 30, 2009
    Date of Patent: September 24, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Waldemar Pfrengle, Thorsten Pachur
  • Patent number: 8541587
    Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.
    Type: Grant
    Filed: April 4, 2012
    Date of Patent: September 24, 2013
    Assignee: Amira Pharmaceuticals, Inc.
    Inventors: Thomas Jon Seiders, Jeffrey Roger Roppe, Timothy Andrew Parr
  • Patent number: 8536175
    Abstract: The invention relates to compounds of formula (I) wherein the substituens are as defined in the specification, in free form or in the form of a pharmaceutically acceptable salt, solvate, ester, N-oxide thereof; processes for the preparation thereof; to pharmaceuticals containing such compounds, in particular for the use in one or more Protein tyrosine kinase mediated diseases.
    Type: Grant
    Filed: August 16, 2012
    Date of Patent: September 17, 2013
    Assignee: Novartis AG
    Inventors: Pascal Furet, Diana Graus Porta, Vito Guagnano
  • Patent number: 8536173
    Abstract: The invention relates to compounds of formula (I), where A, Ar1, Ar2, R1a, R1b, R1c, R2a, R2b, R2c, R3, R4 and R8 are as described herein, and pharmaceutical compositions thereof, methods of preparation thereof, and methods of use thereof.
    Type: Grant
    Filed: July 23, 2010
    Date of Patent: September 17, 2013
    Assignee: SANOFI
    Inventors: Olivier Crespin, Eric Nicolai, Olivier Venier
  • Patent number: 8530473
    Abstract: The invention relates to a compound of the general formula (I), as defined herein which is useful in modulating the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) and are useful for treating pathologies in which such modulation is beneficial, as in the case of metabolic syndrome or of noninsulin-dependent type 2 diabetes. The invention also relates to pharmaceutical preparations containing such a compound, processes for preparing and intermediates useful in the preparation of a such a compound.
    Type: Grant
    Filed: July 23, 2010
    Date of Patent: September 10, 2013
    Assignee: Sanofi
    Inventors: Claudie Namane, Eric Nicolai, Francois Pacquet, Cecile Pascal, Olivier Venier
  • Patent number: 8518973
    Abstract: A compound having the following formula [I] or a pharmaceutically acceptable salt thereof: wherein A is an aromatic five-membered heterocycle which optionally is fused with a cycloalkane ring; B is an alkylene; R1 and R2 are hydrogen, hydroxyl, alkoxy, aryloxy, alkyl, cycloalkyl, aryl, heterocycle, amino, alkylamino, arylamino or acyl, or R1 and R2 join together to form a heterocycle; X and Y are hydrogen, halogen, hydroxyl, alkoxy, aryloxy, alkyl, cycloalkyl, aryl, mercapto, alkylthio, arylthio, carboxyl, an ester of carboxyl, an amide of carboxyl, cyano or nitro; p is 0, 1 or 2; and q is 0 or 1. The compound is useful for treating diseases in which angiogenesis or augmentation of vascular permeability is involved.
    Type: Grant
    Filed: April 18, 2012
    Date of Patent: August 27, 2013
    Assignee: Santen Pharmaceutical Co., Ltd.
    Inventors: Takahiro Honda, Hisashi Tajima, Yoshimasa Sasabuchi, Kenji Kawashima, Kazuyoshi Okamoto, Minoru Yamamoto, Masakazu Ban
  • Patent number: 8518945
    Abstract: The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables n, p, q, Q, X, X? and Y are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.
    Type: Grant
    Filed: March 4, 2011
    Date of Patent: August 27, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Robert Than Hendricks, Johannes Hermann, Rama Kondru, Yan Lou, Stephen M. Lynch, Timothy D. Owens, Michael Soth
  • Patent number: 8518974
    Abstract: The present invention is concerned with isoxazole-pyridine derivatives of formula I wherein X, R1 to R6 are as described herein. The compounds are active on the GABA A ?5 receptor binding site and useful for the treatment of cognitive disorders, such as Alzheimer's disease.
    Type: Grant
    Filed: February 10, 2012
    Date of Patent: August 27, 2013
    Assignee: Hoffmann-La Roche Inc
    Inventors: Bernd Buettelmann, Roland Jakob-Roetne, Henner Knust, Matthew C. Lucas, Andrew Thomas
  • Patent number: 8513248
    Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein A is hydrogen, C1-4alkyl, C3-6cycloalkyl, C1-3alkoxy, C1-3alkoxy C1-4alkyl, C1-2fluoroalkyl, halogen, NR6R7, optionally substituted heteroaryl (Het), or optionally substituted phenyl, and R1, R2, R3, R4, R5, R6 and R7 are as defined in the description. The compounds or salts are thought to modulate P2X7 receptor function and to be capable of antagonizing the effects of ATP at the P2X7 receptor. The invention also provides the use of the compound or salt in the treatment or prophylaxis of, for example, inflammatory pain, neuropathic pain, visceral pain, rheumatoid arthritis or osteoarthritis or neurodegenerative disorders.
    Type: Grant
    Filed: April 28, 2010
    Date of Patent: August 20, 2013
    Assignee: Glaxo Group Limited
    Inventors: David Kenneth Dean, Jorge Munoz-Muriedas, Mairi Sime, Jon Graham Anthony Steadman, Rachel Elizabeth Anne Thewlis, Giancarlo Trani, Ian David Wall, Daryl Simon Walter
  • Patent number: 8507515
    Abstract: Crystalline forms of imatinib mesylate (F, G, H, I and K) and their respective characterization are disclosed.
    Type: Grant
    Filed: July 15, 2011
    Date of Patent: August 13, 2013
    Assignee: Novartis AG
    Inventor: Michael Mutz
  • Patent number: 8507492
    Abstract: Provided herein are Heteroaryl Compounds having the following structure: wherein R1-R4 are as defined herein, compositions comprising an effective amount of a Heteroaryl Compound and methods for treating or preventing cancer, inflammatory conditions, immunological conditions, neurodegenerative diseases, diabetes, obesity, neurological disorders, age-related diseases, or cardiovascular conditions, comprising administering an effective amount of a Heteroaryl Compound to a patient in need thereof.
    Type: Grant
    Filed: November 14, 2011
    Date of Patent: August 13, 2013
    Assignee: Signal Pharmaceuticals, LLC
    Inventors: Sophie Perrin-Ninkovic, Roy L. Harris, John Sapienza, Graziella Shevlin, Patrick Papa, Branden Lee, Garrick Packard, Lida Tehrani, Jingjing Zhao, Jennifer Riggs, Jason Parnes, Deborah Mortensen, Weiming Xu, Loui Madakamutil, Kimberly Fultz, Rama K. Narla, Sabita Sankar, Jan Elsner
  • Patent number: 8507535
    Abstract: The invention relates to a compound of formula wherein A is defined herein or to pharmaceutically active salts, stereoisomeric forms, including individual diastereoisomers and enantiomers of the compound of formula I as well as racemic and non-racemic mixtures thereof. The present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
    Type: Grant
    Filed: June 29, 2011
    Date of Patent: August 13, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Matthias Nettekoven, Hasane Ratni, Walter Vifian