Chalcogen Or -c(=x)-, Wherein X Is Chalcogen, Attached Directly To The Six Membered Hetero Ring By Nonionic Bonding Patents (Class 546/110)
  • Publication number: 20150038438
    Abstract: The present description relates to compounds and forms and pharmaceutical compositions thereof and methods for use thereof to treat or ameliorate bacterial infections caused by wild-type and multi-drug resistant Gram-negative and Gram-positive pathogens.
    Type: Application
    Filed: August 29, 2012
    Publication date: February 5, 2015
    Inventors: Arthur Branstrom, Vara Prasad Venkata Nagendra Josyula, Michael Andrew Arnold, Aleksey I. Gerasyuto, Gary Karp, Jiashi Wang, Guangming Chen, Olya Ginzburg, Song Huang, Jana Narasimhan, Srinivasa Peddi, Sean Wesley Smith, Anthony Allan Turpoff, Matthew G. Woll, Nanjing Zhang, Xiaoyan Zhang
  • Patent number: 8946260
    Abstract: The present invention provides compounds of Formula (I), or a pharmaceutically acceptable salt thereof, where R1, R2, R3, R4, R5, R6, A and n are as defined herein. A deuteriated derivative of the compound of Formula (I) is also provided.
    Type: Grant
    Filed: September 14, 2011
    Date of Patent: February 3, 2015
    Assignee: Novartis AG
    Inventors: Mark Gary Bock, Christoph Gaul, Venkateshwar Rao Gummadi, Henrik Moebitz, Saumitra Sengupta
  • Publication number: 20140171646
    Abstract: Amorphous and polymorphic of palonosetron hydrochloride are disclosed that can be characterized by X-ray powder diffraction patterns, thermal properties, purity and methods of manufacture. These forms of palonosetron hydrochloride can be produced from solution or by solid state interconversions. The forms can be used in pharmaceutical formulations: particularly preferred uses of these formulations are in prevention and treatment of nausea and emesis arising from chemotherapy or postoperative side effects. The forms can optionally be used as mixtures of the crystalline and/or amorphous forms.
    Type: Application
    Filed: October 2, 2013
    Publication date: June 19, 2014
    Applicant: Helsinn Healthcare S.A.
    Inventors: Waldo MOSSI, Giorgio CALDERARI, Wilma TAMRAZ, Tai Wah CHAN
  • Publication number: 20140045872
    Abstract: The present invention provides compounds of Formula (I), or a pharmaceutically acceptable salt thereof, where R1, R2, R3, R4, R5, R6, A and n are as defined herein. A deuteriated derivative of the compound of Formula (I) is also provided.
    Type: Application
    Filed: September 14, 2011
    Publication date: February 13, 2014
    Applicant: NOVARTIS AG
    Inventors: Mark Gary Bock, Christoph Gaul, Venkateshwar Rao Gummadi, Henrik Moebitz, Saumitra Sengupta
  • Publication number: 20140045793
    Abstract: The present invention provides a quinolone compound that inhibits the chronic progression of Parkinson's disease or protects dopamine neurons from disease etiology, thereby suppressing the progression of neurological dysfunction, so as to prolong the period of time until L-dopa is administered while also improving neuronal function; the quinolone compound of the invention is represented by Formula (1): wherein: R1 represents hydrogen or the like; R2 represents hydrogen or the like; R3 represents substituted or unsubstituted phenyl or the like; R4 represents halogen or the like; R5 represents hydrogen or the like; R6 represents hydrogen or the like; and R7 represents hydrogen or the like.
    Type: Application
    Filed: October 18, 2013
    Publication date: February 13, 2014
    Applicant: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Kenji OTSUBO, Takahito YAMAUCHI, Yuji OCHI
  • Publication number: 20140038999
    Abstract: The present disclosure is generally directed to compounds which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds, and methods for inhibiting AAK1.
    Type: Application
    Filed: July 19, 2013
    Publication date: February 6, 2014
    Inventors: Vivekananda M. Vrudhula, Senliang Pan, Ramkumar Rajamani, Susheel Jethanand Nara, Maheswaran Sivasamban Karatholuvhu, Tarun Kumar Maishal, Jonathan L. Ditta, Carolyn Diane Dzierba, Joanne J. Bronson, John E. Macor
  • Publication number: 20140031544
    Abstract: The present invention relates to compounds defined by formula I wherein the variables R1, R2, R3, R4, and m are defined as in claim 1, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of 11?-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity, and dyslipidemia.
    Type: Application
    Filed: June 20, 2013
    Publication date: January 30, 2014
    Applicants: Boehringer Ingelheim International GmbH, Vitae Pharmaceuticals, Inc.
    Inventors: Matthias Eckhardt, Frank Himmelsbach, Linghang Zhuang, Stefan Peters, Herbert Nar
  • Patent number: 8623521
    Abstract: A heterocyclic compound, an organic light-emitting diode, and a flat display device, the heterocyclic compound being represented by Formula 1, below:
    Type: Grant
    Filed: December 6, 2011
    Date of Patent: January 7, 2014
    Assignee: Samsung Display Co., Ltd.
    Inventors: Young-Kook Kim, Seok-Hwan Hwang, Hye-Jin Jung, Jin-O Lim, Sang-Hyun Han, Yoon-Hyun Kwak, Sun-Young Lee, Hee-Joo Ko, Jong-Hyuk Lee, Sung-Chul Kim
  • Patent number: 8617722
    Abstract: The present invention provides a polymer material capable of preparing organic EL elements having low driving voltage and high durability. The polymer compound of the present invention includes a constituting unit derived from a monomer represented by the formula (1); (in the formula (1), each of A1's is independently a condensed polycyclic aromatic group optionally having a heteroatom as a ring-constituting atom; the condensed polycyclic aromatic group links to A2 at the meta position to the bonding position of the ring represented by the following formula; each of A2's is independently a six-membered ring aromatic group optionally having a heteroatom as a ring-constituting atom; at least one of A1 and A2 has a substituent having a polymerizable functional group; at least one of X's is a nitrogen atom, and n's are independently 1 or 2).
    Type: Grant
    Filed: February 20, 2009
    Date of Patent: December 31, 2013
    Assignee: Showa Denko K.K.
    Inventors: Masahiko Toba, Tsuyoshi Kato
  • Patent number: 8614011
    Abstract: An electroluminescent material comprises the following structural unit: where X is selected from a group consisting of NR, O, S, SO, SO2, CR2, PR, POR, BR, SiR2; where R is a substituent group and Ar1 and Ar2 comprise aromatic rings; and, wherein Ar1 or Ar2 is fused to a further aryl system Ar3. An optical device comprises a first electrode for injection of positive charge carriers, a second electrode for injection of negative charge carriers and a layer located between the first and second electrode comprising the electroluminescent material.
    Type: Grant
    Filed: July 23, 2009
    Date of Patent: December 24, 2013
    Assignees: Cambridge Display Technology Limited, Sumitomo Chemical Co., Ltd.
    Inventors: Annette Steudel, Thomas Pounds
  • Publication number: 20130178612
    Abstract: Chiral auxiliaries useful for efficiently producing a phosphorus atom-modified nucleic acid derivative with high stereoregularity, and compounds represented by the following the general formula (I) or the general formula (XI) for introducing the chiral auxiliaries.
    Type: Application
    Filed: September 22, 2011
    Publication date: July 11, 2013
    Applicant: CHIRALGEN, LTD.
    Inventors: Takeshi Wada, Mamoru Shimizu
  • Publication number: 20130005675
    Abstract: The present invention provides a quinolone compound that inhibits the chronic progression of Parkinson's disease or protects dopamine neurons from disease etiology, thereby suppressing the progression of neurological dysfunction, so as to prolong the period of time until L-dopa is administered while also improving neuronal function; the quinolone compound of the invention is represented by Formula (1): wherein: R1 represents hydrogen or the like; R2 represents hydrogen or the like; R3 represents substituted or unsubstituted phenyl or the like; R4 represents halogen or the like; R5 represents hydrogen or the like; R6 represents hydrogen or the like; and R7 represents hydrogen or the like.
    Type: Application
    Filed: September 14, 2012
    Publication date: January 3, 2013
    Applicant: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Kenji OTSUBO, Takahito YAMAUCHI, Yuji OCHI
  • Patent number: 8334298
    Abstract: Disclosed herein is a method for preventing ovarian hyperstimulation syndrome in a subject by administering an effective amount of a dopamine agonist in a pharmaceutically acceptable carrier. Also disclosed herein is a method for treating ovarian hyperstimulation syndrome by administering an effective amount of a dopamine agonist in a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: April 24, 2006
    Date of Patent: December 18, 2012
    Assignee: Ferring International Center S.A.
    Inventors: Antonio Pellicer-Martinez, Joan-Carles Arce, Carlos Simon-Valles, Raul Gomez-Gallego
  • Patent number: 8293899
    Abstract: The present invention relates to a process for preparing stereoisomerically enriched 3-heteroaryl-3-hydroxycarboxylic esters by reducing 3-heteroaryl-3-oxocarboxylic esters in the presence of ruthenium-containing catalysts.
    Type: Grant
    Filed: February 27, 2003
    Date of Patent: October 23, 2012
    Assignee: Lanxess Deutschland GmbH
    Inventors: Boris Bosch, Markus Eckert, Hans-Christian Militzer, Claus Dreisbach
  • Patent number: 8288387
    Abstract: The present invention provides the compounds of general formula 5 and 9 useful as potential antitumour agents against human cancer cell lines. The present invention further provides the process for preparation of napthalimide-benzimidazole hybrids of general formula 5 and 9, n-1-2, R=n-methylpiperazine or morpholine (Formula 9), wherein: n=2-3, m=2-3 and R=n-methylpiperazine or morpholine.
    Type: Grant
    Filed: March 3, 2009
    Date of Patent: October 16, 2012
    Assignee: Council of Scientific & Industrial Research
    Inventors: Kamal Ahmed, Praveen Kumar Pogula
  • Publication number: 20120245194
    Abstract: The present invention is directed to novel compounds that are able to inhibit the interaction of paxillin or its paralogues, including leupaxin or Hic-5, with alpha.4 integrin or its binding partners that regulate signaling events downstream of the paxillin-alpha.4 interaction. The present invention further relates to methods for therapeutic use of such compounds and pharmaceutical compositions of such compounds for the treatment of a disease or condition.
    Type: Application
    Filed: September 15, 2010
    Publication date: September 27, 2012
    Applicant: University of California Technology Transfer
    Inventors: Mark Ginsberg, Christiane Kummer
  • Publication number: 20120157403
    Abstract: Heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salt or solvate of said compound, isomer or racemic mixture wherein represents an optional double bond, the dotted line is optionally a bond or no bond, resulting in a double bond or a single bond, as permitted by the valency requirement and wherein E, A, G M, Het, B, X, R3, R10, R11, R32 and R33 are herein defined and the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.
    Type: Application
    Filed: February 24, 2012
    Publication date: June 21, 2012
    Inventors: Samuel Chackalamannil, Mariappan V. Chelliah, Yuguang Wang, Yan Xia
  • Patent number: 8183238
    Abstract: Compounds of Formula X: wherein A, X, Y, Z, R5, R6a, and R6b are as defined herein, and pharmaceutically acceptable salts thereof, are described as useful for the treatment of cognitive deficits associated with schizophrenia and other neurodegenerative and/or neurological disorders in mammals, including humans.
    Type: Grant
    Filed: June 16, 2010
    Date of Patent: May 22, 2012
    Assignee: Pfizer Inc.
    Inventors: Michelle M. Claffey, Amy B. Dounay, Matthew M. Hayward, Suobao Rong, Patrick R. Verhoest, Jamison B. Tuttle, Xinmin Gan
  • Publication number: 20120108581
    Abstract: The present invention provides a low molecular weight compound having EPO production-promoting action and/or hemoglobin production-promoting action. The present invention relates to a fused piperidine compound represented by the following general formula (1): (wherein, ring A represents a C10-14 aryl group or 5- to 10-membered heterocyclic group, X represents N—R7, a sulfur atom or an oxygen atom, R1, R2, R2?, R3 and R3? independently represent a hydrogen atom, C1-6 alkyl group or C3-6 cycloalkyl group, and R4, R5 and R6 independently represent a hydrogen atom or halogen atom), or a salt thereof, or a solvate thereof.
    Type: Application
    Filed: March 25, 2010
    Publication date: May 3, 2012
    Applicant: Kowa Company, Ltd
    Inventors: Masanori Ashikawa, Toshiharu Morimoto, Hajime Yamada, Shunji Takemura, Tatsuaki Nishiyama, Takeshi Doi, Hiroyuki Ishiwata
  • Publication number: 20110312918
    Abstract: The present invention provides a novel mechanistic pathway and methods related to this pathway for the identification of compounds for the treatment of diseases involving cell proliferation, invasion and/or metastasis such as cancer. In particular, the instant invention relates to the phosphatase activity of Eya and the Eya-Six complex as a target for identifying novel therapeutic agents for the treatment of proliferative, invasive and/or metastatic disorders, and compositions identified using the methods disclosed herein.
    Type: Application
    Filed: December 8, 2009
    Publication date: December 22, 2011
    Applicant: Children's Hospital Medical Center
    Inventor: Rashmi Hegde
  • Patent number: 8071588
    Abstract: The present invention relates to novel compounds of Formula (I) and their use in the treatment of respiratory diseases, including anti-inflammatory and allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rhinitis (e.g. allergic rhinitis), atopic dermatitis or psoriasis.
    Type: Grant
    Filed: February 5, 2009
    Date of Patent: December 6, 2011
    Assignee: Glaxo Group Limited
    Inventors: James Francis Callahan, Guoliang Lin, Zehong Wan, Hongxing Yan
  • Publication number: 20110269967
    Abstract: Novel amic acids and amic esters can be thermally converted into corresponding arylene diimides. These amic acids and amic ester can be used as precursors to prepare semiconducting thin films that can be used in various articles including thin-film transistor devices that can be incorporated into a variety of electronic devices. In this manner, the arylene diimides need not be coated out of solvent in which they may be insoluble, but they can be generated in situ from a solvent-soluble, easily coated amic acid or amic ester.
    Type: Application
    Filed: April 30, 2010
    Publication date: November 3, 2011
    Inventors: Deepak Shukla, Dianne M. Meyer, Wendy G. Ahearn
  • Patent number: 8039474
    Abstract: The invention relates to novel tetrahydro-1H-carbazole derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and methods of treatment comprising administration of said compounds to patients.
    Type: Grant
    Filed: December 22, 2005
    Date of Patent: October 18, 2011
    Assignee: Actelion Pharmaceutical Ltd.
    Inventors: Anja Fecher, Heinz Fretz, Markus Riederer
  • Publication number: 20110136800
    Abstract: The present invention relates to compounds defined by formula I wherein the variables R1, R2, R3, R4, and m are defined as in claim 1, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of 11?-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity, and dyslipidemia.
    Type: Application
    Filed: November 5, 2010
    Publication date: June 9, 2011
    Inventors: Matthias Eckhardt, Stefan Peters, Herbert Nar, Frank Himmelsbach, Linghang Zhuang
  • Patent number: 7923521
    Abstract: The present invention describes a process for the preparation of homoleptic and heteroleptic tris-ortho-metallated metal compounds which are used as coloring components as functional materials in a number of different applications which can be ascribed to the electronics industry in the broadest sense.
    Type: Grant
    Filed: November 9, 2006
    Date of Patent: April 12, 2011
    Assignee: Merck Patent GmbH
    Inventors: Philipp Stoessel, Rocco Fortte, Amir Parham, Esther Breuning, Holger Heil, Horst Vestweber
  • Publication number: 20100324043
    Abstract: Compounds of Formula X: wherein A, X, Y, Z, R5, R6a, and R6b are as defined herein, and pharmaceutically acceptable salts thereof, are described as useful for the treatment of cognitive deficits associated with schizophrenia and other neurodegenerative and/or neurological disorders in mammals, including humans.
    Type: Application
    Filed: June 16, 2010
    Publication date: December 23, 2010
    Inventors: Michelle M. Claffey, Amy B. Dounay, Matthew M. Hayward, Suobao Rong, Patrick R. Verhoest, Jamison B. Tuttle, Xinmin Gan
  • Publication number: 20100004277
    Abstract: Disclosed are compositions and methods for modulating protein trafficking and treating or preventing disorders characterized by impaired protein trafficking. Also disclosed are methods for identification of compounds that rescue protein trafficking defects and methods of enhancing protein production.
    Type: Application
    Filed: January 26, 2007
    Publication date: January 7, 2010
    Applicant: FoldRx Pharmaceuticals, Inc.
    Inventors: Christine Bulawa, Michael DeVit
  • Publication number: 20090270414
    Abstract: The invention relates to novel tetrahydro-1H-carbazole derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and methods of treatment comprising administration of said compounds to patients.
    Type: Application
    Filed: December 22, 2005
    Publication date: October 29, 2009
    Applicant: Actelion Pharmaceuticals Ltd.
    Inventors: Anja Fecher, Heinz Fretz, Markus Riederer
  • Publication number: 20090258852
    Abstract: The instant invention provides for compounds which comprise benzoisoquinolinones and aza derivatives that inhibit CHK1 activity. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting CHK1 activity by administering the compound to a patient in need of treatment of cancer.
    Type: Application
    Filed: June 30, 2006
    Publication date: October 15, 2009
    Inventors: Kenneth L. Arrington, Vadim Y. Dudkin, Mark E. Fraley, Robert M. Garbaccio, George D. Hartman, Shaei Y. Huang, Constantine Kreatsoulas, Edward S. Tasber
  • Publication number: 20090069564
    Abstract: The present invention relates to the field of anti-inflammatory substances, and more particularly to novel compounds that act as antagonists of the mammalian adhesion proteins known as selectins. In some embodiments, methods for treating selectin mediated disorders are provided which include administration of compound of Formula I: wherein the constituent variables are defined herein.
    Type: Application
    Filed: November 7, 2008
    Publication date: March 12, 2009
    Applicant: Wyeth
    Inventors: Neelu Kaila, Silvano L. Debernardo, Kristin M. Janz, Raymond T. Camphausen, Patricia W. Bedard, Adrian Huang
  • Publication number: 20080266647
    Abstract: A colorant molecule is provided that includes at least one switch unit. The switch unit comprises ring-based tautomers, of which there may be more than one per chromophore, and may include donor and/or acceptor moieties.
    Type: Application
    Filed: April 26, 2007
    Publication date: October 30, 2008
    Inventors: Kent D. Vincent, Xian-An Zhang, Zhou-Lin Zhou
  • Publication number: 20080171874
    Abstract: This invention relates to a method for the regioselective synthesis of 4,6,7,8-substituted benzo[g]quinoline-3-carbonitriles and 4,6,7,8-substituted benzo[g]quinazolines as well as intermediates thereof. The compounds derived from this invention are useful for the treatment of a variety of diseases that are a result of deregulation of these PTK's, and more specifically, are anti-cancer agents and are useful for the treatment of cancer in mammals. In addition, the compounds derived from this invention are useful for the treatment of polycystic kidney disease in mammals.
    Type: Application
    Filed: March 24, 2008
    Publication date: July 17, 2008
    Applicant: Wyeth
    Inventors: Dan Maarten Berger, Gary Harold Birnberg, Yanyong Wang
  • Patent number: 7205311
    Abstract: This invention pertains to certain acridone and acridine compounds of the formula which inhibit telomerase, regulate cell proliferation, etc., and/or treat cancer, proliferative conditions, etc.
    Type: Grant
    Filed: January 14, 2003
    Date of Patent: April 17, 2007
    Assignee: Cancer Research Technology Limited
    Inventors: Stephen Neidle, Richard John Harrison, Lloyd Royston Kelland, Sharon Michele Gowan, Martin Anthony Read, Anthony Reszka
  • Patent number: 7145011
    Abstract: The invention relates to a method for the production of substituted 1,2,3,4-tetrahydroquinoline-2-carboxylic acids, i.e. 7,9-dichlor-3a,4,5,9b-tetrahydro-3H-cyclopental[c]quinoline-4-carboxylic acid.
    Type: Grant
    Filed: July 22, 2004
    Date of Patent: December 5, 2006
    Assignee: Grunenthal GmbH
    Inventor: Michael Thomas Przewosny
  • Patent number: 7129093
    Abstract: A method of determining beryllium or a beryllium compound thereof in a sample, includes providing a sample suspected of comprising beryllium or a compound thereof, extracting beryllium or a compound thereof from the sample by dissolving in a solution, adding a fluorescent indicator to the solution to thereby bind any beryllium or a compound thereof to the fluorescent indicator, and determining the presence or amount of any beryllium or a compound thereof in the sample by measuring fluorescence.
    Type: Grant
    Filed: March 30, 2004
    Date of Patent: October 31, 2006
    Assignee: Los Alamos National Security, LLC
    Inventors: T. Mark McCleskey, Deborah S. Ehler, Kevin D. John, Anthony K. Burrell, Gavin E. Collis, Edel M. Minogue, Benjamin P. Warner
  • Patent number: 7109327
    Abstract: The invention relates to a method for the synthesis of galanthamifle, the derivatives and analogues thereof of formula (1) where R1=a hydrogen atom.
    Type: Grant
    Filed: June 14, 2002
    Date of Patent: September 19, 2006
    Assignee: Centre National de la Recherche Scientifique (CNRS)
    Inventors: Claude Thal, Catherine Guillou, Jean-Luc Beunard, Emmanuel Gras, Pierre Potier
  • Patent number: 7012144
    Abstract: Quinolone carboxylic acid derivatives of formula (I) and pharmaceutically acceptable salts thereof have potent antibacterial activity: wherein, R1 is a C1-4 alkyl group, or phenyl or C3-6 cycloalkyl group optionally substituted with one or more halogens; R2 is H, amino or C1-4 alkyl group; R3 is H, C1-4 alkyl group, or amino, aminomethyl or aminoethyl group optionally substituted with one C1-4 alkyl radical; W is N, CH or CY (Y is halogen, or C1-4 alkyl or C1-4 alkoxy group optionally substituted with one or more halogens); and Pyr represents 2-, 3- or 4-pyridyl group, provided that when W is C, W and R1 are fused together to form COCH2CH(CH3), CCH2CH2CH(CH3), or CSCH2CH(CH3).
    Type: Grant
    Filed: December 27, 2002
    Date of Patent: March 14, 2006
    Assignee: Korea Research Institute of Chemical Technology
    Inventors: Tae-Ho Park, Sang-Ho Lee, Cheol Han
  • Patent number: 6991858
    Abstract: The present invention relates to a blue light-emitting compound for organic polymer EL devices and organic EL devices having superior color purity and light-emitting efficiency by providing a blue light-emitting compound for organic EL devices represented by Chemical Formula 1 and an organic EL device using the blue light-emitting compound: wherein R1 to R8 each independently represents a functional group selected from the group consisting of hydrogen alkyl groups, alkoxy groups, carbon rings, aryl groups, hetero rings and fused aromatic compounds having from 1 to 30 carbon atoms; to of R1 to R3 may additionally be connected by a ring; and two of R4 to R8 may additionally be connected by a ring.
    Type: Grant
    Filed: February 4, 2003
    Date of Patent: January 31, 2006
    Assignee: Samsung SDI Co., Ltd.
    Inventors: Kwan Hee Lee, Soo Jin Park, Jong In Hong, Kyung Sun Choi, Chan Hyo Lee, Dae Yup Shin, Dong Hyun Jung, Sang Hyun Ju, Jang Hyuk Kwon
  • Patent number: 6958347
    Abstract: The present invention provides NPY-5 receptor antagonists having a Formula (I) Methods and pharmaceutical compositions useful for treating diseases, conditions and/or disorders modulated by the above NPY-5 receptor antagonists are also provided.
    Type: Grant
    Filed: December 1, 2003
    Date of Patent: October 25, 2005
    Assignee: Pfizer Inc.
    Inventor: Marlys Hammond
  • Patent number: 6894061
    Abstract: This invention provides a compound of formulae (I) or (II) having the structure or a pharmaceutically acceptable salt thereof which are useful for the treatment of the inflammatory component of diseases and are particularly useful in treating atherosclerosis, myocardial infarction, congestive heart failure, inflammatory bowel disease, arthritis, type II diabetes, and autoimmune diseases such as multiple sclerosis and rheumatiod arthritis.
    Type: Grant
    Filed: November 20, 2003
    Date of Patent: May 17, 2005
    Assignee: Wyeth
    Inventors: Albert John Molinari, Mark Antony Ashwell, Brian Hugh Ridgway, Amedeo Arturo Failli, William Jay Moore
  • Patent number: 6833455
    Abstract: Disclosed herein are bridged perinones/quinophthalones of the general formula (I) or tautomeric forms thereof where X1, X2, Ar1 Ar2 and B are as described herein and are particularly characterized in that the bridging B is a radical of the formula —T1—W—T2—, where T1 and T2 are independently O or S and W is alkylene, especially C1-C6-alkylene, C6-C10-arylene, especially phenylene or cycloalkylene, which are each optionally substituted or is the radical of the formula (a) where the phenyl rings are optionally substituted and A is a radical of the formula O, S, SO, SO2 or CO, optionally substituted alkylene, or optionally substituted cycloalkylene, said alkylene or cycloalkylene being attached to the adjacent phenyl rings itself or else via its substitutents, or W is a radical of the formulae where s and t are independently from 1 to 6, the ends of the radical B each being attached to an aromatic carbon atom of the two radicals Ar1
    Type: Grant
    Filed: November 22, 2002
    Date of Patent: December 21, 2004
    Assignee: Bayer Aktiengesellschaft
    Inventors: Christoph Thiebes, Josef-Walter Stawitz, Ulrich Feldhues
  • Publication number: 20040167155
    Abstract: This invention provides a compound of formulae (I) or (II) having the structure 1
    Type: Application
    Filed: November 20, 2003
    Publication date: August 26, 2004
    Inventors: Albert John Molinari, Mark Antony Ashwell, Brian Hugh Ridgway, Amedeo Arturo Failli, William Jay Moore
  • Publication number: 20040152719
    Abstract: The present invention relates to inhibition of viruses, e.g., HIV using quinolones and compounds related to quinolones. The invention further relates to methods for identifying and using agents, including small molecule chemical compositions that inhibit HIV in a cell; as well as to methods of prophylaxis, and therapy related to HIV infection and related disease states such as AIDS.
    Type: Application
    Filed: October 21, 2003
    Publication date: August 5, 2004
    Applicant: IRM LLC, a Delaware LLC
    Inventors: Yun He, David Archer Ellis, Beth Marie Anaclerio, Kelli L. Kuhen, Baogen Wu, Tao Jiang
  • Patent number: 6699899
    Abstract: Imido and amido substituted acylhydroxamic acids which reduce the levels of TNF&agr; and inhibit phosphodiesterase in a mammal. A typical embodiment is (3-(1,3-dioxoisoindolin-2-yl)-3-(3-ethoxy-4-methoxyphenyl)propanoylamino)propanoate.
    Type: Grant
    Filed: December 21, 1999
    Date of Patent: March 2, 2004
    Assignee: Celgene Corporation
    Inventors: Hon-Wah Man, George W Muller, Shaei Y Huang
  • Publication number: 20030225274
    Abstract: The present invention relates to a process for preparing stereoisomerically enriched 3-heteroaryl-3-hydroxycarboxylic esters by reducing 3-heteroaryl-3-oxocarboxylic esters in the presence of ruthenium-containing catalysts.
    Type: Application
    Filed: February 27, 2003
    Publication date: December 4, 2003
    Inventors: Boris Bosch, Markus Eckert, Hans-Christian Militzer, Claus Dreisbach
  • Publication number: 20030105123
    Abstract: N-oxides of the compounds of formula (I) in which R1 is hydroxyl, 1-4C-alkoxy, 3-7C-cycloalkoxy, 3-7C-cycloalkylmethoxy or completely or predominantly fluorine-substituted 1-4C-alkoxy, R2 is hydroxyl, 1-4C-alkoxy, 3-7C-cycloalkoxy, 3-7C-cycloalkylmethoxy or completely or predominantly fluorine-substituted 1-4C-alkoxy, or in which R1 and R2 together are a 1-2C-alkylenedioxy group, R6 is an R7- and R8-substituted phenyl radical, they are active bronchial therapeutics.
    Type: Application
    Filed: June 18, 2002
    Publication date: June 5, 2003
    Inventor: Beate Schmidt
  • Patent number: 6559308
    Abstract: The present invention relates to a method for preparing quinoxaline-5- and 6-carboxylic acids. The method comprises contacting an aqueous suspension of a 5- or 6-hydroxymethyl quinoxaline with oxygen in the presence of a transition metal catalyst, to form the respective quinoxaline-5- or 6-carboxylic acid. The method for oxidizing benzylic methyl groups may also be employed to prepare a wide variety of heterocyclic carboxylic acid compounds.
    Type: Grant
    Filed: August 9, 2001
    Date of Patent: May 6, 2003
    Assignee: Air Products and Chemicals, Inc.
    Inventor: Juan Jesus Burdeniuc
  • Patent number: 6303569
    Abstract: The present invention is directed to double prodrugs containing polymeric-based transport forms.
    Type: Grant
    Filed: August 21, 1998
    Date of Patent: October 16, 2001
    Assignee: Enzon, Inc.
    Inventors: Richard B. Greenwald, Yun H. Choe, Annapurna Pendri
  • Patent number: 6288232
    Abstract: The invention pertains to a method for preparing derivatives of the pyrazolinylnaphthalic acid having the general formula where Ar1 and Ar2 are unsubstituted or substituted phenyl radicals bearing in the para position an alkylated or acylated oxy- or amino group, or a polynuclear aryl radical, and Ar3 is a substituted N-naphthalimid or 1,8-naphthylene-1′,2′-benzimidazole. Compounds of the above general formula are high-efficient red organic luminophors and are used widely as luminescent components of dyes for plastics and liquid scintillators, in hydrogeology to study water streams, to label the chemical industry wastewaters, as laser dyes, etc.
    Type: Grant
    Filed: December 21, 2000
    Date of Patent: September 11, 2001
    Assignee: eMagin Corporation
    Inventors: Victor M. Shershukov, Valentina T. Skripkina
  • Patent number: RE41366
    Abstract: The invention relates to a method for the synthesis of galanthamine, the derivatives and analogues thereof of formula (1) where R1=a hydrogen atom, R2=a hydroxy group, R1 and R2 together form ?O, R3, R4, and R5 independently=a hydrogen atom, a hydroxy group or a (C1-C2)alkoxy group, R6?H, (C1-C12)alkyl, (CH2)nNR7R8, or —(CH2)nN+R7R8R9 where n=1 to 12, Z=two hydrogen atoms, or an oxygen atom and X=an oxygen, sulphur or nitrogen atom, or a —SO, —SO2, or —NR6 group where R6 is as defined above or is an amine protecting group.
    Type: Grant
    Filed: June 14, 2002
    Date of Patent: June 1, 2010
    Assignee: Centre National del la Recherche Scientifique (CNRS)
    Inventors: Claude Thal, Catherine Guillou, Jean-Luc Beunard, Emmanuel Gras, Pierre Potier