Nitrogen Patents (Class 562/430)
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Patent number: 11359183Abstract: The present invention provides engineered transaminase polypeptides useful for the synthesis of chiral amine compounds under industrially relevant conditions. The invention also provides polynucleotides encoding the engineered transaminase polypeptides, host cells capable of expressing the engineered transaminases, and methods of using the engineered transaminases for the production of chiral amine compounds.Type: GrantFiled: May 23, 2018Date of Patent: June 14, 2022Assignee: Codexis, Inc.Inventors: Scott J. Novick, Nikki Dellas, Oscar Alvizo, Ravi David Garcia, Charlene Ching, David Entwistle
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Publication number: 20150148544Abstract: A compound of the general formula X—[NR—CO—Ar—CO—(CH?CH)n—(CH2)2-L]m (I) in which X represents a polymer; R represents a hydrogen atom or an alkyl, aryl or alkyl-aryl group; Ar represents an unsubstituted or substituted heteroaryl or aryl group; n represents 0 or an integer of from 1 to 4; L represents a leaving group; and m represents an integer of from 1 to 8. The compounds find use in the conjugation of biological molecules.Type: ApplicationFiled: February 4, 2015Publication date: May 28, 2015Inventor: Antony Godwin
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Publication number: 20150141513Abstract: The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for the treatment of neurological degenerative disorders and neurological diseases may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of narcolepsy, shift work sleep disorder, and as an adjunct treatment for obstructive sleep apnea/hypopnea, hypersomnias, like idiopathic hypersomnia, Psychiatric/neurodegenerative disorders, ADHD, Psychiatric/neurodegenerative disorders, Depersonalization disorder, Cognitive enhancement, Fatigue, Post-chemotherapy cognitive impairment and weight loss.Type: ApplicationFiled: April 19, 2013Publication date: May 21, 2015Inventor: Mahesh Kandula
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Publication number: 20150094276Abstract: This invention relates to novel substituted styryl benzylsulfones that are multikinase inhibitors and pharmaceutically acceptable acid addition salts thereof. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by an agent that inhibits kinases, such as phosphatidylinositol 3-kinase (PI3-K) and polo-like kinase (PLK-1).Type: ApplicationFiled: April 19, 2013Publication date: April 2, 2015Inventor: Roger D. Tung
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Patent number: 8993780Abstract: The present invention relates to novel amide derivatives of N-urea substituted amino acids, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.Type: GrantFiled: December 10, 2013Date of Patent: March 31, 2015Assignee: Allergan, Inc.Inventors: Richard L. Beard, Tien T. Duong, John E. Donello, Veena Viswanath, Michael E. Garst
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Publication number: 20150038708Abstract: In one aspect, the invention relates to substituted 2-hydroxy-4-(2-(phenylsulfonamido)acetamido)benzoic acid analogs, derivatives thereof, and related compounds, which are useful as inhibitors of STAT protein activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders of uncontrolled cellular proliferation associated with a STAT protein activity dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: August 5, 2014Publication date: February 5, 2015Inventors: James Turkson, Patrick Gunning
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Patent number: 8933267Abstract: The present invention relates to a compound according to formula I in particular as anti-ulcer agent and/or anti-Helicobacter pylori agent, wherein R1 is selected from linear or branched C1-C6 alkyl, H, thioether and benzyl, and R2 is selected from linear or branched C1-C10 alkanediyl and pharmaceutical compositions thereof.Type: GrantFiled: March 13, 2014Date of Patent: January 13, 2015Assignee: King Saud UniversityInventors: Amani S. Awaad, Reham Moustafa El-Meligy, Ahmed M. Alafeefy
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Patent number: 8895746Abstract: The present invention provides compounds S3I-201.1066 (Formula 1) and S3I-201.2096 (Formula 2) as selective Stat3 binding agents that block Stat3 association with cognate receptor pTyr motifs, Stat3 phosphorylation and nuclear translocation, Stat3 transcriptional function, and consequently induced Stat3-specific antitumor cell effects in vitro and antitumor response in vivo.Type: GrantFiled: November 10, 2013Date of Patent: November 25, 2014Assignees: University of Central Florida Research Foundation, Inc., The Governing Council of the University of TorontoInventors: James Turkson, Patrick Gunning
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Publication number: 20140329778Abstract: The present invention relates to a compound according to formula I in particular as anti-ulcer agent and/or anti-Helicobacter pylori agent, wherein R1 is selected from linear or branched C1-C6 alkyl, H, thioether and benzyl, and R2 is selected from linear or branched C1-C10 alkanediyl and pharmaceutical compositions thereofType: ApplicationFiled: March 13, 2014Publication date: November 6, 2014Applicant: King Saud UniversityInventors: Amani S. AWAAD, Reham Moustafa EL-MELIGY, Ahmed M. ALAFEEFY
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Patent number: 8822467Abstract: The present invention provides biaryl oxyacetic acid compounds which may be useful for treating inflammatory disorders, including disorders affecting the respiratory system and skin.Type: GrantFiled: December 14, 2012Date of Patent: September 2, 2014Assignee: Ligand Pharmaceuticals IncorporatedInventors: Brian F. McGuinness, Koc-Kan Ho, Suresh Babu, Guizhen Dong, Jingqi Duo, Thuy X. H. Le, Kurt W. Saionz
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Publication number: 20140228325Abstract: The present invention relates to alkene derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.Type: ApplicationFiled: February 6, 2014Publication date: August 14, 2014Applicant: Allergan, Inc.Inventors: Wenkui K. Fang, Ken Chow, Evelyn G. Corpuz
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Publication number: 20140194416Abstract: The invention relates to N-hydroxylsulfonamide derivatives that donate nitroxyl (HNO) under physiological conditions and are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure and ischemia/reperfusion injury. Novel N-hydroxylsulfonamide derivatives release NHO at a controlled rate under physiological conditions, and the rate of HNO release is modulated by varying the nature and location of functional groups on the N-hydroxylsulfonamide derivatives.Type: ApplicationFiled: March 11, 2014Publication date: July 10, 2014Applicants: Cardioxyl Pharmaceuticals, Inc., The Johns Hopkins UniversityInventors: John P. Toscano, Frederick Arthur Brookfield, Andrew D. Cohen, Stephen Martin Courtney, Lisa Marie Frost, Vincent Jacob Kalish
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Publication number: 20140128469Abstract: The present invention provides a compound of Formula I: as defined herein, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: May 8, 2012Publication date: May 8, 2014Applicant: CONCERT PHARMACEUTICALS INC.Inventor: Roger Tung
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Publication number: 20140094466Abstract: In alternative embodiments, the invention provides compositions that inhibit the polypeptide SSH-2, or SlingSHot-2, a phosphatase enzyme that regulates actin filaments, and methods for making and using them, including methods comprising administering compositions of the invention to regulate or modify actin filament polymerization by inhibiting SSH-2, where in one embodiment compositions of the invention slow or inhibit F-actin depolymerization and severing. In alternative embodiments, compositions and methods of the invention are used to slow or inhibit cell motility and/or internal remodeling. In alternative embodiments, compositions and methods of the invention are used to slow or inhibit, or reverse, or ameliorate the progression of a cancer or a metastasis or other uncontrolled or unregulated cell growth, and/or Alzheimer's disease.Type: ApplicationFiled: March 15, 2012Publication date: April 3, 2014Inventors: Jason H. Haga, Shu Chien, Matt Mui, Marshall J. Levesque, Phillip D. Pham
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Publication number: 20140094614Abstract: The present invention relates to novel amide derivatives of N-urea substituted amino acids, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.Type: ApplicationFiled: December 10, 2013Publication date: April 3, 2014Applicant: Allergan, Inc.Inventors: Richard L. Beard, Tien T. Duong, John E. Donello, Veena Viswanath, Michael E. Garst
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Publication number: 20140094455Abstract: Compounds, including 3-carboxy aryl sulfonamide compounds, which agonize or antagonize aquaporin channels and methods of using them to treat disorders or diseases mediated by aquaporins.Type: ApplicationFiled: August 19, 2013Publication date: April 3, 2014Applicant: ARIZONA BOARD OF REAGENTS ON BEHALF OF THE UNIVERSITY OF ARIZONAInventors: Gary A. Flynn, Andrea J. Yool, Elton Rodrigues Migliati, Leslie S. Ritter
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Patent number: 8686154Abstract: Carrier compounds and compositions therewith which are useful in the delivery of active agents are provided. Methods of administration and preparation are provided as well.Type: GrantFiled: June 10, 2009Date of Patent: April 1, 2014Assignee: Emisphere Technologies, Inc.Inventors: Donald J. Sarubbi, Eugene N. Barantsevitch
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Patent number: 8658803Abstract: The present invention relates to novel amide derivatives of N-urea substituted amino acids, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.Type: GrantFiled: October 23, 2012Date of Patent: February 25, 2014Assignee: Allergan, Inc.Inventors: Richard L. Beard, Tien T. Duong, John E. Donello, Veena Viswanath, Michael E. Garst
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Publication number: 20140024717Abstract: The present invention relates to a process for the preparation of the mono sodium salt of the derivative 3,5-diiodo-O-[3-iodo-4-(sulphooxy)phenyl]-L-tyrosine (T3S) by starting from the corresponding phenolic compound, in the presence of chloro-sulfonic acid and dimethylacetamide as a solvent. The so obtained T3S compound may conveniently be isolated in a pure form as a solid in good yields. The present invention further relates to the process for T3S preparation, wherein the starting reagent is T2 and further comprising the formulation of such compound in tablets. Furthermore, the invention discloses non-radioactive immunoassays based on T3S derivatives.Type: ApplicationFiled: April 5, 2012Publication date: January 23, 2014Applicant: BRACCO IMAGING S.p.A.Inventors: Pier Lucio Anelli, Maria Argese, Luciano Lattuada, Federico Maisano, Sonia Gazzetto, Laura Galimberti, Valeria Boi, Giovanni Rivolta, Livio Cavalieri, Fulvia Vella
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Publication number: 20140011129Abstract: A polymerizable monomer is provided which is represented by the following formula (1): wherein R1 represents a hydrogen atom or an alkyl group; A represents —CO— or —SO2—; and the moiety represented by the formula (1) is, at the part shown by an asterisk *, linked to a moiety represented by the following formula (2), at any position of a, b, c or d thereof; wherein the sites among a, b, c and d at which the moiety represented by the formula (2) is not linked to the moiety represented by the formula (1) each has a hydrogen atom or a substituent selected from the group consisting of an alkyl group, an alkoxy group and a sulfonic acid group, or any of which may connect at mutually adjoining positions to form a ring.Type: ApplicationFiled: March 27, 2012Publication date: January 9, 2014Applicant: CANON KABUSHIKI KAISHAInventors: Yasuaki Murai, Kei Inoue, Ryuji Murayama, Kazuyuki Sato, Masashi Hirose
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Publication number: 20140011130Abstract: To provide a polymeric compound having superior charge-providing properties, the polymeric compound contains at least one unit represented by the following general formula (5). In the general formula (5), R1 represents a hydrogen atom or an alkyl group; R2 to R4 each represent a hydrogen atom, an alkyl group, an alkoxy group, a hydroxyl group or a halogen atom, or R3 and R4 may combine each other to form a ring; and A represents a divalent linking group.Type: ApplicationFiled: March 27, 2012Publication date: January 9, 2014Applicant: CANON KABUSHIKI KAISHAInventors: Kei Inoue, Yasuaki Murai, Ryuji Murayama, Kazuyuki Sato, Soichiro Kawakami, Masashi Hirose
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Publication number: 20130331450Abstract: Disclosed are compositions and methods for treating bacterial infections.Type: ApplicationFiled: March 15, 2013Publication date: December 12, 2013Applicant: Purdue Research FoundationInventors: Cynthia Stauffacher, Mark Alfred Lipton, Mohamed Naguieb Saleem, Tim Jonathan Schmidt, Calvin Nicklaus Steussy, JR., Victor W. Rodwell
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Patent number: 8586749Abstract: The present invention provides compounds S3I-201.1066 (Formula 1) and S3I-201.2096 (Formula 2) as selective Stat3 binding agents that block Stat3 association with cognate receptor pTyr motifs, Stat3 phosphorylation and nuclear translocation, Stat3 transcriptional function, and consequently induced Stat3-specific antitumor cell effects in vitro and antitumor response in vivo.Type: GrantFiled: April 5, 2010Date of Patent: November 19, 2013Assignees: University of Central Florida Research Foundation, Inc., Governing Council of the University of TorontoInventors: James Turkson, Patrick Gunning
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Patent number: 8524194Abstract: The invention is directed to radiolabelled MMP selective compounds, a processes for the preparation thereof, and uses thereof. The derivatives of the invention have formula (I) wherein Y represents O, CH2, (CH2)2, S, NH, or C(?O)NH; X represents 1-5 substituents, wherein said substituents can be the same or different and wherein at least one of said substituents comprises a radioisotope suitable for PET and/or SPECT and/or a ?-emitter; Z is S; Q is chosen from the group consisting of 3-pyridyl and carboxyl; and R is chosen from the group consisting of C(?O)—NH—OH, (II), (III, (IV). The MMP selective compounds of the invention are selective for MMPs and can be used for the identification and treatment of unstable atherosclerotic plaques.Type: GrantFiled: May 14, 2009Date of Patent: September 3, 2013Assignee: Academisch Medisch Centrum Bij de Universiteit van AmsterdamInventors: Bertha Louise Frederike Van Eck-Smit, Victorine Augustine Pinas, Albert Dirk Windhorst
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Publication number: 20130225621Abstract: In one aspect, the invention relates to substituted 2-hydroxy-4-(2-(phenylsulfonamido)acetamido)benzoic acid analogs, derivatives thereof, and related compounds, which are useful as inhibitors of STAT protein activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders of uncontrolled cellular proliferation associated with a STAT protein activity dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: August 2, 2011Publication date: August 29, 2013Applicants: University of Toronto Mississauga, University of Central Florida Research Foundation, Inc.Inventors: James Turkson, Patrick Gunning
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Publication number: 20130217652Abstract: The present invention relates to novel thiobenzyl and sulfinylbenzyl derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.Type: ApplicationFiled: February 20, 2013Publication date: August 22, 2013Applicant: ALLERGAN, INC.Inventor: ALLERGAN, INC.
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Publication number: 20130203727Abstract: The invention provides compounds of formula (I): or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula (I), intermediates useful for preparing compounds of formula I and therapeutic methods for treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds of formula (I).Type: ApplicationFiled: July 1, 2011Publication date: August 8, 2013Applicant: GILEAD SCIENCES, INC.Inventors: Kerim Babaoglu, Elizabeth Bacon, Kyla Bjornson, Hongyan Guo, Randall L. Halcomb, Paul Hrvatin, John O. Link, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Paul Roethle, James Taylor, James D. Trenkle, Randall W. Vivian, Lianhong Xu
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Patent number: 8501242Abstract: The present invention relates to compounds as novel thymidylate synthase inhibitors, novel strategies to treat or prevent neoplasia in a subject, methods and compositions thereof.Type: GrantFiled: May 29, 2010Date of Patent: August 6, 2013Assignee: University of Florida Research FoundationInventors: David A. Ostrov, Carmen J. Allegra
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Publication number: 20130190338Abstract: The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.Type: ApplicationFiled: March 11, 2013Publication date: July 25, 2013Applicant: ALLERGAN, INC.Inventor: ALLERGAN, INC.
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Publication number: 20130190370Abstract: The present invention relates to TP receptor antagonists, which have the ability to bind to TP receptor and optionally cross the blood brain barrier. The invention also provides compositions and methods for treating a disorder wherein activation of TP receptor is detrimental.Type: ApplicationFiled: July 27, 2011Publication date: July 25, 2013Applicant: The Trustees of the University of PennsylvaniaInventors: John Q. Trojanowski, Virginia M.Y. Lee, Kurt R. Brunden, Amos B. Smith, Donna M. Huryn, Carlo Ballatore, Anne-Marie Hogan, Francesco Piscitelli
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Publication number: 20130183252Abstract: The present invention relates to the discovery that specific human taste receptors in the T2R taste receptor family respond to particular bitter compounds present in, e.g., coffee. Also, the invention relates to the discovery of specific compounds and compositions containing that function as bitter taste blockers and the use thereof as bitter taste blockers or flavor modulators in, e.g., coffee and coffee flavored foods, beverages and medicaments. Also, the present invention relates to the discovery of a compound that antagonizes numerous different human T2Rs and the use thereof in assays and as a bitter taste blocker in compositions for ingestion by humans and animals.Type: ApplicationFiled: February 10, 2012Publication date: July 18, 2013Applicant: Senomyx, Inc.Inventors: Xiaodong LI, Andrew Patron, Catherine Tachdjian, Hong Xu, Qing Li, Alexey Pronin, Guy Servant, Lan Zhang, Thomas Brady, Vincent Darmohusodo, Melissa Arellano, Victor Selchau, Brett Weylan Ching, Donald S. Karanewsky, Paul Brust, Jing Ling, Wen Zhao, Chad Priest
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Patent number: 8445706Abstract: An unnatural amino acid including a phosphate mimicking group for mimicking a phosphate group in phosphoamino acids and a protein phosphatase modifying group for covalently binding protein phosphatases. A probe for detecting disease including a phosphate mimicking group for mimicking a phosphate group in phosphoamino acids and a protein phosphatase modifying group for covalently binding protein phosphatases. A method for detecting the presence of disease by administering the unnatural amino acid, binding the unnatural amino acid with a phosphatase, detecting a signal, and detecting the presence of disease. A method of identifying a known protein phosphatase, and a method of identifying an unknown protein phosphatase. A method of making the unnatural amino acid.Type: GrantFiled: September 1, 2009Date of Patent: May 21, 2013Assignee: Board of Trustees of Northern Illinois UniversityInventor: Kui Shen
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Publication number: 20130109866Abstract: The present invention relates to novel amide derivatives of N-urea substituted amino acids, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.Type: ApplicationFiled: October 23, 2012Publication date: May 2, 2013Applicant: ALLERGAN, INC.Inventor: ALLERGAN, INC.
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Publication number: 20130102609Abstract: The present invention provides biaryl oxyacetic acid compounds which may be useful for treating inflammatory disorders, including disorders affecting the respiratory system and skin.Type: ApplicationFiled: December 14, 2012Publication date: April 25, 2013Applicant: LIGAND PHARMACEUTICALS INC.Inventor: Ligand Pharmaceuticals Inc.
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Publication number: 20130096127Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R5, B1, X and n are defined herein. The invention also relates a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: November 29, 2012Publication date: April 18, 2013Applicant: NOVARTIS AGInventor: NOVARTIS AG
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Publication number: 20130096319Abstract: The present invention is related to a novel process for the preparation of amisulpride (I) which involves: methylation of 4-amino-salicylic-acid (VI) with dimethyl sulphate and base, optionally in presence of TBAB to obtain 4-amino-2-methoxy methyl benzoate (VII) and (ii) oxidation of 4-amino-2-methoxy-5-ethyl thio benzoic acid (IX) or 4-amino-2-methoxy-5-ethyl thio methyl benzoate (X) with oxidizing agent in the presence of sodium tungstate or ammonium molybdate to give 2-methoxy-4-amino-5-ethyl-sulfonyl benzoic acid (IV) or 2-methoxy-4-amino-5-ethyl-sulfonyl methyl benzoate (XI) respectively.Type: ApplicationFiled: June 9, 2011Publication date: April 18, 2013Applicant: Lupin LimitedInventors: Dinesh Jayntibhai Paghdar, Mahesh Ramkumar Kolekar, Tushar Nandkumar Deshpande, Suryaprakash Pandurang Patil, Yuvraj Atmaram Chavan, Purna Chandra Ray, Girij Pal Singh
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Publication number: 20130046103Abstract: The present invention provides several synthetic methods for preparing N-(2-butylbenzofuran-5-yl)-N-(methylsulfonyl)methanesulfonamide, a compound of formula (3), an intermediate in the preparation of Dronedarone. The present invention further provides a process for preparing Dronedarone, comprising the steps of converting 2-butyl-5-bis(methanesulfon)-amidobenzofuran of formula (3) to Dronedarone, wherein the 2-butyl-5-bis(methanesulfon)-amidobenzofuran of formula (3) is prepared by the processes of the present invention.Type: ApplicationFiled: February 10, 2011Publication date: February 21, 2013Applicant: MAPI PHARMA LIMITEDInventors: Ehud Marom, Michael Mizhiritskii, Shai Rubnov
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Publication number: 20120289554Abstract: This invention relates to novel 4-dimethylaminobutyric acid derivatives of the formula wherein A1, A2, R1, m and n are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds inhibit carnitine palmitoyl transferase (CPT) activity, in particular CPT2 activity, and can be used as medicaments in methods for the treatment of diseases modulated by CPT2 inhibitors.Type: ApplicationFiled: July 24, 2012Publication date: November 15, 2012Inventors: Mirjana Andjelkovic, Simona M. Ceccarelli, Odile Chomienne, Gerald Lewis Kaplan, Patrizio Mattei, Jefferson Wright Tilley
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Publication number: 20120282180Abstract: The present invention relates to the field of therapeutic and diagnostic agents and more specifically to compounds of formula (I) that are inhibitors of matrix-metalloproteinases (MMPs) and are useful in the treatment of diseases related thereto such as cardiovascular diseases, inflammatory diseases and malignant diseases. One embodiment of the invention is a compound of formula (I) labeled with a 18-fluorine atom having matrix metalloproteinase inhibitory activity suitable for diagnostic imaging. Also disclosed in the present invention is a pharmaceutical composition comprising the inhibitors of matrix-metalloproteinases (MMPs) of the invention or the corresponding labeled compounds useful as diagnostic imaging agents of the invention in a form suitable for mammalian administration.Type: ApplicationFiled: June 8, 2011Publication date: November 8, 2012Inventors: Hartmuth C. Kolb, Guenter Haufe, Malte Behrends, Klaus Kopka, Stefan Wagner, Verena Hugenberg, Hans-Joerg Breyholz, Sven Hermann, Michael Schaefers
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Publication number: 20120263714Abstract: The present invention relates to substituted halophenoxybenzamide derivative compounds of general formula (I) in which R1, R2, R3, R3a, R4, R5, R6, Ra, Rb, Rc, and X are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.Type: ApplicationFiled: October 12, 2010Publication date: October 18, 2012Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Marion Hitchcock, Ingo Hartung, Florian Pühler, Gerhard Siemeister, Roland Neuhaus
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Publication number: 20120252894Abstract: The invention relates to a compound which inhibits the importation of chloride into neurons or a compound which improve the outflow of chloride from neurons thereby promoting the inhibitory actions of GABA and alleviating pain and stress of the fetus during delivery and the newborn. The invention also relates to a pharmaceutical composition for use in a method for alleviating pain and stress of the fetus during delivery and the newborn comprising a compound according to the invention and a pharmaceutically acceptable carrier.Type: ApplicationFiled: March 30, 2012Publication date: October 4, 2012Inventors: Giniatullin Rashid, Khazipov Roustem, Ben-Ari Yehezkel, Mazzuca Michel, Tyzio Roman
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Publication number: 20120252997Abstract: Fluorinated arylene-containing compounds and fluorinated polymers formed from fluorinated arylene-containing compounds, and methods are described. Fluorinated polymers formed from fluorinated arylene-containing compound can be used to provide a low energy surface.Type: ApplicationFiled: December 17, 2010Publication date: October 4, 2012Inventors: Yu Yang, George G.I. Moore, John C. Clark
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Patent number: 8268885Abstract: The present invention relates to small molecules as entry inhibitors of the HIV virus, processes for their preparation as well as pharmaceutical compositions, their use as medicines, and diagnostic kits comprising them. The present invention also concerns combinations of the present entry inhibitors with other anti-retroviral agents. It further relates to their use in assays as reference compounds or as reagents. The compounds of the present invention are useful for preventing or treating infection by HIV and for treating AIDS.Type: GrantFiled: September 10, 2004Date of Patent: September 18, 2012Assignee: Janssen R&D IrelandInventors: Koenraad Lodewijk August Van Acker, Piet Tom Bert Paul Wigerinck, Lieve Emma Jan Michiels, Abdellah Tahri
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Publication number: 20120232104Abstract: The invention is concerned with novel sulfonamide derivatives of formula (I) wherein R2, R3, R4, A, X, Y1, Y2, Y3, Y4 and Z1 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used as medicaments.Type: ApplicationFiled: May 22, 2012Publication date: September 13, 2012Inventors: Konrad Bleicher, Simona Maria Ceccarelli, Odile Chomienne, Patrizio Mattei, Tanja Schulz-Gasch, Christoph Martin Stahl
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Patent number: 8247602Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions that include the compounds described herein, and methods of using such antagonists of PGD2 receptors, alone or in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.Type: GrantFiled: September 27, 2011Date of Patent: August 21, 2012Assignee: Panmira Pharmaceuticals, LLCInventors: John Howard Hutchinson, Thomas Jon Seiders, Jeannie M. Arruda
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Publication number: 20120208988Abstract: Compounds of Formula (Ia) wherein R is a C6-C12 substituted or unsubstituted aryl, a C6-C12 substituted or unsubstituted heteroaryl, a C1-C6 substituted or unsubstituted alkyl or —NR?R?, Q is C(O), O, NR?, S, S(O)2, C(O)2 (CH2)p Y is C(O), O, NR?, S, S(O)2, C(O)2 (CH2)p Z is H or C1-C4 alkyl, R? is H, C(O), S(O)2, C(O)2, a C6-C12 substituted or unsubstituted aryl, a C6-C12 substituted or unsubstituted heteroaryl or a C1-C6 substituted or unsubstituted alkyl, when substituted, aryl, heteroaryl and alkyl are substituted with halogen, C6-C12 heteroaryl, —NR?R? or COOZ, which have diagnostic and therapeutic properties, such as the treatment and management of prostate cancer and other diseases related to NAALADase inhibition. Radiolabels can be incorporated into the structure through a variety of prosthetic groups attached at the X amino acid side chain via a carbon or hetero atom linkage.Type: ApplicationFiled: November 11, 2011Publication date: August 16, 2012Applicant: MOLECULAR INSIGHTS PHARMACEUTICALS, INC.Inventors: John W. Babich, Craig N. Zimmerman, Kevin P. Maresca
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Patent number: 8242118Abstract: The present invention relates to a sulfonamide derivative which is useful as an active ingredient of pharmaceutical preparations. The sulfonamide derivatives of the present invention have CCR3 (CC type chemokine receptor) antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with CCR3 activity, in particular for the treatment of asthma, atopic dermatitis, allergic rhinitis and other inflammatory/immunological disorders.Type: GrantFiled: April 19, 2010Date of Patent: August 14, 2012Assignee: Axikin Pharmaceuticals Inc.Inventors: Yingfu Li, Akihiko Watanabe, Timothy B. Lowinger, Kevin Bacon, Norihiro Kawamura, Takuya Shintani, Tetsuo Kikuchi, Toshiya Moriwaki, Klaus Urbahns, Keiko Fukushima, Noriko Nunami, Takashi Yoshino, Toshiki Murata, Megumi Yamauchi, Hiroko Yoshino
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Publication number: 20120202854Abstract: Compounds of formula (I): in which R1, R2, R7, R8, R9, R10 and A have the meanings given in the specification, are DP2 receptor modulators useful in the treatment of immunologic diseases.Type: ApplicationFiled: April 17, 2012Publication date: August 9, 2012Applicant: ARRAY BIOPHARMA INC.Inventors: George Doherty, Adam Cook
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Publication number: 20120196933Abstract: The present invention concerns prodrugs of mexiletine (and mexiletine's active metabolite) pharmaceutical compositions containing such prodrugs. Methods for treating myotonic conditions, while reducing the inherent adverse GI side effects associated with mexiletine, increasing the bioavailability of mexiletine, and improving the pharmacokinetic reproducibility of mexiletine with the aforementioned prodrugs are also provided.Type: ApplicationFiled: December 22, 2011Publication date: August 2, 2012Inventors: Richard Franklin, Bernard T. Golding, Robert G. Tyson
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Publication number: 20120164097Abstract: Bad odors on textile materials are often caused by body odor. The invention relates to a textile material treatment method for inhibiting body odor on textile materials, by which means the treated textiles, after having been worn, even after sweat-inducing sports activities, have a significantly reduced bad odor or even no odor. The invention also relates to a perfume composition and to a textile material treatment agent, respectively comprising urea derivatives and/or phenacylthiazolium salts, that counteract the formation of body odor.Type: ApplicationFiled: March 8, 2012Publication date: June 28, 2012Applicant: Henkel AG & Co. KGaAInventors: Ursula Huchel, Markus Egert, Andreas Bauer, Andreas Gerigk, Frank Pessel