Nitrogen Attached Indirectly To The Tetrazole Ring By Nonionic Bonding Patents (Class 548/254)
  • Patent number: 9115132
    Abstract: The present invention relates to novel tetrazole compounds of Formula (I) wherein A is (II) or (III); to processes for their preparation; to pharmaceutical compositions containing the compounds; and to the use of the compounds in therapy to treat diseases for which blocking the Cav2.2 calcium channels is beneficial.
    Type: Grant
    Filed: July 8, 2011
    Date of Patent: August 25, 2015
    Assignee: Convergence Pharmaceuticals Limited
    Inventors: Paul Beswick, Robert James Gleave, Shuji Hachisu, Sadie Vile, Nicholas Bertheleme, Simon E. Ward
  • Publication number: 20150087821
    Abstract: The present invention provides a new method for isolation and/or purification of immunoglobulins from a solution containing one or more immunoglobulins using a solid phase matrix represented by the formula: M-SP-L, wherein M is designates a matrix backbone, SP designates a spacer and L designates a substituted benzimidazole ligand.
    Type: Application
    Filed: December 5, 2014
    Publication date: March 26, 2015
    Inventors: Gordon R. Duffin, Victoria Jane Dolan, Katherine Louise Angus, Andrew Lyddiatt
  • Patent number: 8987473
    Abstract: The present invention relates to a compound that has URAT1 inhibitory action, and a URAT1 inhibitor, a blood uric acid level-reducing agent and a pharmaceutical composition comprising the compound. More specifically, the present invention relates to a compound represented by Formula (I) below.
    Type: Grant
    Filed: January 30, 2012
    Date of Patent: March 24, 2015
    Assignee: Sato Pharmaceutical Co., Ltd.
    Inventors: Keita Nagai, Koh Nagasawa, Hirobumi Takahashi, Motoaki Baba, Shinichi Fujioka, Eri Kondoh, Kenichi Tanaka, Yoshiki Itoh
  • Patent number: 8962580
    Abstract: The invention features compounds of formula I or II: In one embodiment, the invention relates compounds and processes for conjugating ligand to oligonucleotide. The invention further relates to methods for treating various disorders and diseases such as viral infections, bacterial infections, parasitic infections, cancers, allergies, autoimmune diseases, immunodeficiencies and immunosuppression.
    Type: Grant
    Filed: September 23, 2009
    Date of Patent: February 24, 2015
    Assignee: Alnylam Pharmaceuticals, Inc.
    Inventors: Muthiah Manoharan, Kallanthottathil G. Rajeev, Takeshi Yamada, David Butler, Narayanannair K. Jayaprakash, Muthusamy Jayaraman, Shigeo Matsuda, Rajendra K. Pandey, Chang Geng Peng
  • Publication number: 20150045557
    Abstract: The present invention provides a compound characterized by being represented by general formula (I): (wherein, A represents a halogen atom, alkyl group, haloalkyl group, alkoxy group, haloalkoxy group, alkylsulfonyl group, unsubstituted or substituted aryl group, cyano group or nitro group, n represents an integer of 0 to 5 (and A may be mutually the same or different when n is 2 or more), Y represents an alkyl group, M represents an alkaline metal or alkaline earth metal, and m represents an integer of 1 or 2).
    Type: Application
    Filed: March 6, 2013
    Publication date: February 12, 2015
    Applicant: Nippon Soda Co., Ltd.
    Inventors: Keiichiro Matsuda, Masayuki Matsushita, Kaoru Noda, Satoshi Kajita
  • Publication number: 20140378459
    Abstract: [Problem] Provided is a compound which is useful as an agent for preventing and/or treating renal diseases. [Means for Solution] The present inventors have conducted extensive studies on compounds having a trypsin inhibitory action, and as a result, they have found that a guanidinobenzoic acid compound has a trypsin inhibitory action, thereby completing the present invention. The guanidinobenzoic acid compound of the present invention can be used as an agent for preventing and/or treating renal disease as an agent which will substitute low-protein diet therapy, and an agent for preventing and/or treating trypsin-related diseases, for example, pancreatitis, gastroesophageal reflux disease, hepatic encephalopathy, influenza, and the like.
    Type: Application
    Filed: September 14, 2012
    Publication date: December 25, 2014
    Applicant: ASTELLAS PHARMA INC.
    Inventors: Jiro Fujiyasu, Kazuhiko Ohne, Susumu Yamaki, Tomoyoshi Imaizumi, Takeshi Hondo, Keisuke Matsuura, Tomohki Satou, Satoshi Sasamura
  • Patent number: 8691856
    Abstract: The present invention discloses novel compounds of Formula (I), or pharmaceutically acceptable salts thereof, which have glucagon receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of using them to treat diabetic and other glucagon related metabolic disorders, and the like.
    Type: Grant
    Filed: November 16, 2006
    Date of Patent: April 8, 2014
    Assignee: Eli Lilly and Company
    Inventors: Scott Eugene Conner, Philip Arthur Hipskind, Jianke Li, Guoxin Zhu
  • Patent number: 8680270
    Abstract: The presently disclosed subject matter is directed to metallo-oxidoreductase inhibitors having metal binding moities linked to a targeting moiety through a linking group or a direct bond, methods for screening for metallo-oxidoreductase inhibitors, and methods of treating an oxidoreductase related disorder by administering a metallo-oxidoreductase inhibitor to a subject in need of treatment thereof.
    Type: Grant
    Filed: November 21, 2007
    Date of Patent: March 25, 2014
    Assignee: Viamet Pharmaceuticals, Inc.
    Inventors: Robert J. Schotzinger, William J. Hoekstra
  • Publication number: 20140051857
    Abstract: A compound represented by the formula (1): wherein A is a nitrogen atom or CR4, B is an oxygen atom, a sulfur atom or NR9 (provided that when A is a nitrogen atom, B is not NH), R1 is a C2-14 aryl group, L1 is a bond, CR10R11, an oxygen atom, a sulfur atom or NR12, X is OR13, SR13 or NR14NR15, R2 is a hydrogen atom, a formyl group, a C1-10 alkyl group or the like, L2 is a bond or the like, L3 is a bond, CR17R18, an oxygen atom, a sulfur atom or NR19, L4 is a bond, CR20R21, an oxygen atom, a sulfur atom or NR22, Y is an oxygen atom, a sulfur atom or NR23, and R3 is a C2-14 aryl group, a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.
    Type: Application
    Filed: October 28, 2013
    Publication date: February 20, 2014
    Applicant: Nissan Chemical Industries Limited
    Inventors: Shingo OWADA, Shunsuke Iwamoto, Kazufumi Yanagihara, Katsuaki Miyaji, Takanori Nakamura, Norihisa Ishiwata, Yutaka Hirokawa
  • Publication number: 20140024680
    Abstract: The invention relates to novel arylpyrroline compounds of formula (I) which have excellent insecticidal activity and which can thus be used as an insecticide.
    Type: Application
    Filed: January 9, 2013
    Publication date: January 23, 2014
    Applicant: Bayer Intellectual Property GmbH
    Inventor: Bayer Intellectual Property GmbH
  • Publication number: 20140011997
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
    Type: Application
    Filed: September 12, 2013
    Publication date: January 9, 2014
    Applicant: THERAVANCE, INC.
    Inventors: Cameron Smith, Melissa Fleury, Roland Gendron, Ryan Hudson, Adam D. Hughes
  • Publication number: 20140005221
    Abstract: The present invention relates to a compound that has URAT1 inhibitory action, and a URAT1 inhibitor, a blood uric acid level-reducing agent and a pharmaceutical composition comprising the compound. More specifically, the present invention relates to a compound represented by Formula (I) below.
    Type: Application
    Filed: January 30, 2012
    Publication date: January 2, 2014
    Applicant: SATO PHARMACEUTICAL CO., LTD.
    Inventors: Keita Nagai, Koh Nagasawa, Hirobumi Takahashi, Motoaki Baba, Shinichi Fujioka, Eri Kondoh, Kenichi Tanaka, Yoshiki Itoh
  • Patent number: 8563586
    Abstract: The present invention provides novel 1,5 and 1,3,5-substituted imidazole compounds in hydrophilic or lipophilic form, which are useful as angiotensin II ATI receptor antagonists suitable for transdermal delivery. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing compounds and their use in methods of treating hypertension and cardiovascular diseases.
    Type: Grant
    Filed: May 23, 2008
    Date of Patent: October 22, 2013
    Assignee: Eldrug S.A.
    Inventors: John Matsoukas, Michael Maragoudakis, Dimitrios Vlaxakos
  • Patent number: 8546374
    Abstract: A compound having Formula (I) or Formula (II) is disclosed as an P2X7 antagonist, wherein A, B, C, Y, Y, Z, m, v, R1, R2, R3, R4, and R5, are as defined in the description. Methods and compositions for treating disease or condition modulated by P2X7 are also disclosed.
    Type: Grant
    Filed: July 9, 2012
    Date of Patent: October 1, 2013
    Assignee: Abbvie Inc.
    Inventors: William A. Carroll, Arturo Perez-Medrano, Alan S. Florjancic, Derek W. Nelson, Sridhar Peddi, Tongmei Li, Eric M. Bunnelle, Gavin Hirst, Biquin C. Li
  • Publication number: 20130217702
    Abstract: The present invention relates to the indole derivatives of formula (I), wherein R1-R6 and X are defined in the claims and optical antipodes or racemates and/or salts thereof which are selective antagonists of bradykinin B1 to process for producing these compounds, pharmacological compositions containing them and to their use in therapy or prevention of painful and inflammatory conditions.
    Type: Application
    Filed: November 4, 2011
    Publication date: August 22, 2013
    Inventors: Gyula Beke, Gyula Attila Bényei, István Borza, Éva Bozó, Sándor Farkas, Katalin Hornok, Andrea Papp, István Vágó, Mónika Vastag
  • Publication number: 20130210796
    Abstract: The present invention relates to novel tetrazole compounds; to processes for their preparation; to pharmaceutical compositions containing the compounds; and to the use of the compounds in therapy to treat diseases for which blocking the Cav2.2 calcium channels is beneficial.
    Type: Application
    Filed: July 8, 2011
    Publication date: August 15, 2013
    Inventors: Paul Beswick, Robert James Gleave, Shuji Hachisu, Sadie Vile, Nicholas Bertheleme, Simon E. Ward
  • Publication number: 20130123315
    Abstract: The present invention relates to compounds of the general structure shown in Formula (A): (A): and includes pharmaceutically acceptable salts, solvates, esters, prodrugs, tautomers, and isomers of said compounds. Pharmaceutical compositions and methods of treatment are also included.
    Type: Application
    Filed: July 8, 2011
    Publication date: May 16, 2013
    Inventors: Duane DeMong, Michael W. Miller, Xing Dai, Andrew Stamford
  • Patent number: 8404730
    Abstract: Racemic or enantiomerically enriched 3-substituted propanamine compounds represented by the following structural formula (I): or a pharmaceutically acceptable salt thereof are disclosed. Pharmaceutical compositions containing the subject compounds are also disclosed. The subject compounds are useful for the treatment of diseases of the central nervous system, such as depression, anxiety and pain disorders.
    Type: Grant
    Filed: October 19, 2011
    Date of Patent: March 26, 2013
    Assignee: SK Biopharmaceuticals Co., Ltd.
    Inventors: Chun-Eung Park, Kyung-Hyun Min, Yong-Je Shin, Yu-Jin Shin, Hae-Jeong Yoon, Won Kim, Eun-Ju Ryu, Coo-Min Chung, Hui-Ho Kim
  • Patent number: 8404728
    Abstract: This disclosure relates to materials and methods for inhibiting Botulinum neurotoxin, and more particularly to materials and methods for inhibiting the zinc endopeptidase of Botulinum neurotoxin serotypes A, D and/or E (BoNTA, BoNTD and/or BoNTE).
    Type: Grant
    Filed: July 29, 2010
    Date of Patent: March 26, 2013
    Assignees: Mayo Foundation for Medical Education and Research, U.S. Army Medical Research and Material Command
    Inventors: Yuan-Ping Pang, Jewn Giew Park, Shaohua Wang, Anuradha Vummenthala, Rajesh K Mishra, Jon Davis, Charles B. Millard, James J. Schmidt
  • Patent number: 8362054
    Abstract: Therapeutic compounds, compositions, methods, and medicaments related thereto are disclosed herein.
    Type: Grant
    Filed: February 8, 2008
    Date of Patent: January 29, 2013
    Assignee: Allergan, Inc.
    Inventors: David W. Old, Wha Bin Im, Vinh X. Ngo
  • Publication number: 20130005784
    Abstract: The present invention provides novel pyrazoles that are useful as cannabinoid receptor antagonists and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, and/or cardiometabolic disorders.
    Type: Application
    Filed: December 23, 2011
    Publication date: January 3, 2013
    Applicant: JENRIN DISCOVERY
    Inventors: John F. McElroy, Robert J. Chorvat
  • Publication number: 20120295943
    Abstract: Provided is a therapeutic agent for hyperparathyroidism, renal osteodystrophy, hypercalcemia and the like, which has a CaSR activating (agonist) action. A compound represented by the following general formula (1): [wherein, Ar which is a partial structure in the general formula (1) represents a phenyl group or a naphthyl group; R1a and R1b are the same or different from each other, and represent a hydrogen atom, a halogeno group, or the like; R2a and R2b are the same or different from each other, and represent a hydrogen atom, a halogeno group, or the like; A represents a single bond, an oxygen atom, or the like; B represents a single bond, a C1-C4 alkanediyl group, or the like; Z represents a carboxyl group or a tetrazolyl group; and m represents an integer of 1 to 3] or a pharmacologically acceptable salt thereof.
    Type: Application
    Filed: August 20, 2009
    Publication date: November 22, 2012
    Inventors: Shinji Marumoto, Toyoki Nishimata, Masayuki Ebisawa, Yusuke Asoh, Yasuo Fukushima, Mikio Kato
  • Publication number: 20120289494
    Abstract: Provided herein are compounds, compositions, and methods in the field of medicinal chemistry. The compounds and compositions provided herein relate to spiro-oxindoles which function as antagonists of the interaction between p53 and MDM2, and their use as therapeutics for the treatment of cancer and other diseases.
    Type: Application
    Filed: May 11, 2012
    Publication date: November 15, 2012
    Applicants: Sanofi, The Regents of the University of Michigan
    Inventors: Shaomeng Wang, Wei Sun, Angelo Aguilar, Carlos Garcia-Echeverria
  • Publication number: 20120225873
    Abstract: The invention provides novel compounds useful for the treatment of neurodegenerative disorders including Alzheimer's disease and dementia. The compounds have a substituents chosen from -L-C(?O)OH, -L-CH?CHC(?O)OH, -L-C(?O)NH2, -L-C(?O)NH(C1-3 alkyl), -L-C(?O)N(C1-3 alkyl)2, -L-S(?O)2(C1-3alkyl), -L-S(?O)2NH2, -L-S(?O)2N(C1-3 alkyl)2, -L-S(?O)2NH(C1-3 alkyl), -L-C(?O)NHOH, -L-C(?O)CH2NH2, -L-C(?O)CH2OH, -L-C(?O)CH2SH, -L-C(?O)NHCN, -L-NHC(?O)ORo, -L-C(?O)NHRo, -L-NH(C?O)NHRo, -L-C(?O)N(Ro)2, -L-NH(C?O)N(Ro)2, -L-sulfo, -L-(2,6 difluorophenol), -L-phosphono, and -L-tetrazolyl, where L is a linker.
    Type: Application
    Filed: April 13, 2012
    Publication date: September 6, 2012
    Applicant: Myrexis, Inc.
    Inventors: Rachel Slade, Yevgeniya Klimova, Robert J. Halter, Ashantai J. Yungai, Warren S. Weiner, Ruth J. Walton, Jon Adam Willardsen, Mark B. Anderson, Kenton Zavitz
  • Publication number: 20120196908
    Abstract: This invention describes new antifungal compounds that are aralkyl benzyl ethers of the formula (I): wherein: Ar represents aryl, imidazolil, 1,2,4-triazolyl, benzimidazolil; R1, R2, R4 and R5 are independently hydrogen, halogen, C1-6 alkyl; R3 represents halogen, C1-6alkyl or O—R? where R? represents hydrogen or lower alkyl; R6 represents aryl, substituted aryl, trifluoromethyl, trichloromethyl or O—R? where R? represents hydrogen or lower alkyl; being the substituents of the aryl a halogen or a radical tetrazolyl; n and m represent independently an integer between 0 and 5; With the proviso that when Ar is imidazolil, R3 is chlorine, R6 is p-phenyl and R1, R2, R4 and R5 are hydrogen, n must be different from 2. When n and m are not 0 and 1, R3 or R6 can be represented by substituents not necessarily equal.
    Type: Application
    Filed: August 27, 2010
    Publication date: August 2, 2012
    Applicant: BIOLAB SANUS FARMACEUTICA LTDA.
    Inventors: Artur Franz Keppler, Sérgio Luiz Sacurai, Marcio Henrique Zaim, Carlos Eduardo da Costa Touzarim
  • Patent number: 8207373
    Abstract: HPV inhibitors with formula (I) where G1 represents a hydrocarbonated bond or chain possibly substituted by one or two alkyl groups, G2 represents a group (see formula Ia+Ib) or R represents a hydrogen, an alkyl, halogenoalkyl, or a prodrug radical such as carbamate, acetyl or dialkylaminomethyl, G represents a bond or a hydrocarbonated chain possibly substituted by one or two alkyls, W represents an oxygen or sulphur, R1 and R2 each represent a group chosen from among hydrogen, halogen, hydroxyl, thio, alkoxy, halogenoalkoxy, alkylthio, halogenoalkylthio, amino, monoalkylamino, dialkylamino, cycloalkyl, alkyl or halogenoalkyl, R3 represents an acid or a prodrug radical of the acid function or a bioisostere of the acid function, A represents an aryl, cycloalkyl, cycloalkenyl or a heterocycle, each possibly substituted, and B represents an aryl or a heterocycle with 6 chains, each possibly substituted, and pharmaceutically acceptable salts.
    Type: Grant
    Filed: May 18, 2007
    Date of Patent: June 26, 2012
    Assignee: Anaconda Pharma
    Inventors: Marta Blumenfeld, Delphine Compere, Jean-Michel Gauthier
  • Patent number: 8207183
    Abstract: Novel compounds that inhibit the binding of the Smac protein to Inhibitor of Apoptosis Proteins (IAPs) of the formula (I).
    Type: Grant
    Filed: July 8, 2011
    Date of Patent: June 26, 2012
    Assignee: Novartis AG
    Inventors: Mark G. Palermo, Sushil Kumar Sharma, Christopher Sean Straub, Run-Ming Wang, Leigh Zawel, Yanling Zhang, Zhuoliang Chen, Yaping Wang, Fan Yang, Wojciech Wrona, Gang Liu, Mark G. Charest, Feng He
  • Publication number: 20120149661
    Abstract: The invention relates to tetra-substituted heteroarylic compounds of the formula (I) wherein X1, X3 and X4 are independently C or N, Y is C—H, N—H or N, wherein the total number of nitrogen atoms represented by X1, X3, X4 and Y is 1 or 2; rings A and B are independently selected from phenyl or pyridyl; R1, R4, R?, R?, n and m are as defined herein. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of MDM2 and/or MDM4, or variants thereof.
    Type: Application
    Filed: August 24, 2010
    Publication date: June 14, 2012
    Applicant: NOVARTIS AG
    Inventors: Guido Bold, Pascal Furet, Francois Gessier, Joerg Kallen, Joanna Hergovich Lisztwan, Keiichi Masuya, Andrea Vaupel
  • Publication number: 20120142689
    Abstract: In one aspect, the invention relates to compounds of formula I: where Y, R1, R2, n, and Q are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
    Type: Application
    Filed: December 1, 2011
    Publication date: June 7, 2012
    Applicant: THERAVANCE, INC.
    Inventors: Eric L. STANGELAND, Lori Jean VAN ORDEN, Daisuke Roland SAITO
  • Patent number: 8193368
    Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted tetrazolyl, R2 is optionally substituted phenyl, optionally substituted pyridinyl or optionally substituted thienyl, and R3, R4, R5 and R6 are as defined herein. Also provided are methods of using the compounds for treating diseases associated with the P2X3 and/or a P2X2/3 receptor antagonist and methods of making the compounds.
    Type: Grant
    Filed: August 18, 2009
    Date of Patent: June 5, 2012
    Assignee: Roche Palo Alto LLC
    Inventors: Michael Patrick Dillon, Ronald Charles Hawley, Li Chen, Lichun Feng, Minmin Yang
  • Publication number: 20120122941
    Abstract: Provided is a therapeutic agent for hyperparathyroidism, renal osteodystrophy, hypercalcemia and the like, which has a CaSR activating (agonist) action. A compound represented by the following general formula (1): [wherein, Ar which is a partial structure in the general formula (1) represents a phenyl group or a naphthyl group; R1a and R1b are the same or different from each other, and represent a hydrogen atom, a halogeno group, or the like; R2a and R2b are the same or different from each other, and represent a hydrogen atom, a halogeno group, or the like; A represents a single bond, an oxygen atom, or the like; B represents a single bond, a C1-C4 alkanediyl group, or the like; Z represents a carboxyl group or a tetrazolyl group; and m represents an integer of 1 to 3] or a pharmacologically acceptable salt thereof.
    Type: Application
    Filed: August 20, 2009
    Publication date: May 17, 2012
    Inventors: Shinji Marumoto, Toyoki Nishimata, Masayuki Ebisawa, Yusuke Asoh, Yasuo Fukushima, Mikio Kato
  • Publication number: 20120108635
    Abstract: The invention relates to novel arylpyrroline compounds of formula (I) which have excellent insecticidal activity and which can thus be used as an insecticide.
    Type: Application
    Filed: May 18, 2010
    Publication date: May 3, 2012
    Applicant: Bayer CropScience AG
    Inventors: Tetsuya Murata, Yasushi Yoneta, Hidetoshi Kishikawa, Jun Mihara, Daiei Yamazaki, Mamoru Hatazawa, Norio Sasaki, Kei Domon, Eiichi Shimojo, Teruyuki Ichihara, Katsuhiko Shibuya, Masashi Ataka, Ulrich Görgens
  • Patent number: 8168799
    Abstract: A process for the preparation of a compound of formula (I), or a salt, hydrate or solvate thereof; wherein R1 and R2 are each independently hydrogen, or C1-6 alkyl groups or R1 and R2 are linked and, together with the cyclopentane carbon atoms to which they are attached, form a cyclopropyl ring.
    Type: Grant
    Filed: April 20, 2006
    Date of Patent: May 1, 2012
    Assignee: Merck Sharpe & Dohme Ltd.
    Inventors: Michael Stewart Ashwood, Matthew Bio, Edward Cleator, David Hands, Faye Julia Sheen, Robert Darrin Wilson
  • Publication number: 20120088919
    Abstract: The invention relates to compounds having the formula: wherein: Ar, r, R3, Z, X, and R5-7 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Application
    Filed: December 19, 2011
    Publication date: April 12, 2012
    Applicant: THERAVANCE, INC.
    Inventors: Seok-Ki CHOI, Paul R. FATHEREE, Roland GENDRON, Ryan HUDSON, Robert Murray MCKINNELL, Vivek SASIKUMAR
  • Publication number: 20120038264
    Abstract: The present invention relates to novel carbazole derivatives and an organic light-emitting diode device using the same. These carbazole derivatives can simultaneously or singly be used as a hole transporting layer, a host or guest of an emitting layer or an electron transporting layer of an organic light-emitting diode device.
    Type: Application
    Filed: January 21, 2011
    Publication date: February 16, 2012
    Inventors: Hsiao Chan LIU, Min Sheng Chen, Chin Yi Lee
  • Patent number: 8101642
    Abstract: Racemic or enantiomerically enriched 3-substituted propanamine compounds represented by the following structural formula (I): or a pharmaceutically acceptable salt thereof are disclosed. Pharmaceutical compositions containing the subject compounds are also disclosed. The subject compounds are useful for the treatment of diseases of the central nervous system, such as depression, anxiety and pain disorders.
    Type: Grant
    Filed: June 3, 2009
    Date of Patent: January 24, 2012
    Assignee: SK Biopharmaceuticals Co., Ltd.
    Inventors: Chun-Eung Park, Kyung-Hyun Min, Yong-Je Shin, Yu-Jin Shin, Hae-Jeong Yoon, Won Kim, Eun-Ju Ryu, Coo-Min Chung, Hui-Ho Kim
  • Publication number: 20110301180
    Abstract: It has been discovered that inhibiting mitochondrial respiration in platelets reduces platelet activation or platelet aggregation. Certain heterocyclic compounds significantly reduced one or more platelet functions including clumping, sticking or platelet-stimulated clotting. Thus diseases or disorders mediated by inappropriately high levels of platelet activation or platelet aggregation can be treated by administering a therapeutically effective amount of a heterocyclic compound or nonheterocyclic mitochondrial inhibitor that significantly reduces one or more platelet functions including clumping, sticking or platelet-stimulated clotting, preferably in a reversible manner.
    Type: Application
    Filed: April 25, 2011
    Publication date: December 8, 2011
    Applicant: Stanford University
    Inventors: James P. Collman, Paul Clifford Herrmann, David Alvin Tyvoll, Richard Decreau, Brian Stanley Bull, Christopher Jeffrey Barile
  • Publication number: 20110281875
    Abstract: Novel compounds that inhibit the binding of the Smac protein to Inhibitor of Apoptosis Proteins (IAPs) of the formula (I).
    Type: Application
    Filed: July 8, 2011
    Publication date: November 17, 2011
    Inventors: Mark G. PALERMO, Sushil Kumar SHARMA, Christopher STRAUB, Run-Ming WANG, Leigh ZAWEL, Yanlin ZHANG, Zhuoliang CHEN, Yaping WANG, Fan YANG, Wojciech WRONA, Gang LIU, Mark G. CHAREST, Feng HE
  • Patent number: 8048886
    Abstract: The present invention relates to novel IAP inhibitor compounds of formula I:
    Type: Grant
    Filed: December 7, 2007
    Date of Patent: November 1, 2011
    Assignee: Novartis AG
    Inventors: Zhuoliang Chen, Run-Ming David Wang, Ming Chen, Christopher Sean Straub, Leigh Zawel
  • Patent number: 8048904
    Abstract: The present invention provides a process for the preparation of Olmesartan medoxomil by condensing the ethyl 4-(1-hydroxy-1-methylethyl)-2-propylimidazole-5-carboxylate with 4-[2-(trityl tetrazol-5-yl)phenyl]benzyl bromide to obtain ethyl 4-(1-hydroxy-1-methyl ethyl)-2-propyl-1-{4-[2-(trityl tetrazol-5-yl)phenyl]phenyl}methylimidazole-5-carboxylate and then hydrolyzing ethyl 4-(1-hydroxy-1-methyl ethyl)-2-propyl-1-{4-[2-(trityl tetrazol-5-yl)phenyl]phenyl}methyl imidazole-5-carboxylate to obtain trityl Olmesartan dihydrate followed by reacting trityl Olmesartan dihydrate with 4-chloromethyl-5-methyl-2-oxo-1,3-dioxolene to obtain trityl Olmesartan medoxomil and then deprotecting trityl Olmesartan medoxomil to obtain Olmesartan medoxomil.
    Type: Grant
    Filed: June 15, 2007
    Date of Patent: November 1, 2011
    Assignee: Matrix Laboratories Ltd.
    Inventors: Gorantla Seeta Ramanjaneyulu, Bandari Mohan, Purna Chandra Ray, Madhuresh Kumar Sethi, Vijendra Singh Rawat, Yerramalla Raja Krishna, Vemula Lakshminarayana, Mamidi Srinivas
  • Publication number: 20110251393
    Abstract: The invention provides a helicene derivative, axially chiral amino acid, amine or amino alcohol derivative, and azaperylene, such as compounds represented by Formulae (I), (I?), (II), (II?), and (III): and a method for producing the same.
    Type: Application
    Filed: October 20, 2009
    Publication date: October 13, 2011
    Applicant: KYOTO UNIVERSITY
    Inventors: Takumi Furuta, Takeo Kawabata
  • Patent number: 8026255
    Abstract: This invention is concerned with compounds of the formula and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.
    Type: Grant
    Filed: May 10, 2010
    Date of Patent: September 27, 2011
    Assignee: Hoffman-La Roche Inc.
    Inventors: Alfred Binggeli, Andreas D. Christ, Hans P. Maerki, Rainer E. Martin
  • Publication number: 20110184034
    Abstract: The present invention provides an agent for the prophylaxis or treatment of severe sepsis, which contains a compound represented by the formula (I): or, the formula (II): or a salt thereof or a prodrug thereof, a TLR signal inhibitor containing a non-peptide compound and an agent for the prophylaxis or treatment of organ dysfunction and the like, which contains a TLR signal inhibitory substance.
    Type: Application
    Filed: March 30, 2011
    Publication date: July 28, 2011
    Inventors: Masayuki Ii, Yuji Iizawa, Tomoyuki Kitazaki, Kazuki Kubo
  • Publication number: 20110172212
    Abstract: Novel amine compounds which are represented by the following formula (1) and efficacious against diseases such as a viral infectious disease with HIV, rheumatism, and cancer metastasis; typically, A1 and A2 represent a hydrogen atom or a substitutable monocyclic or polycyclic heteroaromatic ring and W represents a substitutable benzene ring or any group represented by the following formula (10) or (11): where X represents O, CH2, C(?O), NR11, or CHR35 and D represents a group represented by the following formula (6): [Formula 4] -Q-Y—B??(6) where Q represents a single bond, NR12, or a group represented by the formula (13): and Y represents a group represented by the following formula (7): [Formula 6] —(CR18R19)m3- or —(CR20R21)m4-z-(CR22R23)m5-??(7) where z represents a substitutable monocyclic or polycyclic aromatic ring; and B represents —NR25R26; and R1 to R26 in the above formulae represent a hydrogen atom, an alkyl group, an alkenyl group, or an alkynyl group.
    Type: Application
    Filed: March 18, 2011
    Publication date: July 14, 2011
    Applicant: KUREHA CORPORATION
    Inventors: Atsushi SAITOU, Shigeyuki Kikumoto, Masahiro Ono, Ryo Matsui, Masashi Yamamoto, Tomohiro Sawa, Shigeru Suzuki, Mikiro Yanaka
  • Publication number: 20110152295
    Abstract: Heteroaromatic compounds of structural formula I are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis.
    Type: Application
    Filed: September 2, 2009
    Publication date: June 23, 2011
    Inventors: Jean-Philippe Leclerc, Chun Sing Li, Yeeman K. Ramtohul
  • Publication number: 20110152236
    Abstract: The invention relates to compounds of the formula (I) where: R is a (C1-C6)alkyl group, a halo(C1-C6)alkyl group; R1 is a hydrogen atom; R2 is a heteroaromatic group or a heteroaromatic(C1-C4)alkyl group, said groups being optionally substituted; R3 and R4 represent independently from each other an optionally substituted phenyl group; Y is a hydrogen atom, a halogen, a cyano, a (C1-C6)alkyl group, a halo(C1-C6)alkyl group, a (C1-C6)alkoxy group, a halo(C1-C6)alkoxy group or a (C1-C6)alkylS(O)p group; and p is 0 to 2. Said compounds can be in the form— of a base or a salt for addition to an acid. The invention also relates to a method for preparing same and to the therapeutic application thereof.
    Type: Application
    Filed: August 13, 2009
    Publication date: June 23, 2011
    Applicant: SANOFI-AVENTIS
    Inventors: Patrick Bernardelli, Jean-Francois Sabuco, Corinne Terrier
  • Publication number: 20110077279
    Abstract: A compound having the structure wherein R is an angiotensin II receptor antagonist selected from the group consisting of (IIa)-(IIh); A is wherein R1 and R2 are independently selected from the group consisting of hydrogen and C1-4 alkyl. Y is X0—Z wherein X0 is selected from the group consisting of: —O—, —O—CO—, —OCOO—, —OCONH— and —OSO2—; Z is a nitric oxide releasing moiety, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: May 18, 2009
    Publication date: March 31, 2011
    Inventors: Nicoletta Almirante, Massimiliano Ferrario, Silvia Stefanini, Stefano Biondi, Ennio Ongini
  • Publication number: 20110003690
    Abstract: The invention relates to novel arylpyrroline compounds of formula (I) which having excellent insecticidal activity and which can thus be used as an insecticide is provided.
    Type: Application
    Filed: January 29, 2009
    Publication date: January 6, 2011
    Applicant: BAY CROPSCIENCE AG
    Inventors: Ulrich Goergens, Yasushi Yoneta, Tetsuya Murata, Jun Mihara, Kei Domon, Eiichi Shimojo, Katsuhiko Shibuya, Teruyuki Ichihara
  • Patent number: 7855308
    Abstract: The present invention relates to compounds which are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome and other diseases and conditions that are mediated by excessive glucocorticoid action.
    Type: Grant
    Filed: January 19, 2009
    Date of Patent: December 21, 2010
    Assignee: Abbott Laboratories
    Inventors: Michael E. Brune, Peer B. Jacobson, James T. Link, Jyoti R. Patel, Jeffrey J. Rohde, Qi Shuai, Martin Winn, Vince S. Yeh, Hong Yong
  • Publication number: 20100311789
    Abstract: Racemic or enantiomerically enriched 3-substituted propanamine compounds represented by the following structural formula (I): or a pharmaceutically acceptable salt thereof are disclosed. Pharmaceutical compositions containing the subject compounds are also disclosed. The subject compounds are useful for the treatment of diseases of the central nervous system, such as depression, anxiety and pain disorders.
    Type: Application
    Filed: June 3, 2009
    Publication date: December 9, 2010
    Inventors: Chun-Eung Park, Kyung-Hyun Min, Yong-Je Shin, Yu-Jin Shin, Hae-Jeong Yoon, Won Kim, Eun-Ju Ryu, Coo-Min Chung, Hui-Ho Kim