Amino Nitrogen In The Substituent E (i.e.,plural Amino Nitrogens Containing) Patents (Class 564/220)
  • Publication number: 20150045442
    Abstract: Novel melatonin ligands of Formula I: or pharmaceutically acceptable salts thereof wherein: n is 1 or 2; m is 0, 1 or 2; p is 0, 1, 2, 3, 4, 5, 6, 7 or 8; v is 2 or 3; A is aryl or heteroaryl; Z is O, S or NR8; Y is selected from the group consisting of hydrogen, aryl, heteroaryl, C1-C6 alkyl, C3-C6 cycloalkyl, and R is selected from the group consisting of hydrogen, hydroxyl, —OCF3, CF3, C1-C8 alkyl, C1-C8 alkyloxy, C1-C8 alkylthio, halogen and —Z—(CH2)p-A; R1 is selected from the group consisting of C1-C4 alkyl, C3-C6 cycloalkyl, CF3, hydroxy-substituted C1-C4 alkyl, hydroxy-substituted C3-C6 cycloalkyl, and NHR5, wherein R5 is C1-C3 alkyl or C3-C6 cycloalkyl; R2 is selected from the group consisting of: hydrogen, C1-C4 alkyl, C1-C4 alkyloxy, OCF3, CF3, hydroxyl, and halogen; R3 is selected from the group consisting of hydrogen, C1-C4 alkyl, C1-C4 alkyloxy, OCF3, CF3, hydroxyl, and halogen; R and R3 may be connected together to form an —O—(CH2)v bridge representing with the carbon atoms to which the
    Type: Application
    Filed: June 13, 2014
    Publication date: February 12, 2015
    Inventors: Gabriella GOBBI, Marco MOR, Silvia RIVARA, Franco FRASCHINI, Giorgio TARZIA, Annalida BEDINI, Gilberto SPADONI, Valeria LUCINI
  • Patent number: 8791163
    Abstract: Novel melatonin ligands of Formula I: or pharmaceutically acceptable salts thereof wherein: n is 1 or 2; m is 0, 1 or 2; p is 0, 1, 2, 3, 4, 5, 6, 7 or 8; v is 2 or 3; A is aryl or heteroaryl; Z is O, S or NR8; Y is selected from the group consisting of hydrogen, aryl, heteroaryl, C1-C6 alkyl, C3-C6 cycloalkyl, and R is selected from the group consisting of hydrogen, hydroxyl, —OCF3, CF3, C1-C8 alkyl, C1-C8 alkyloxy, C1-C8 alkylthio, halogen and —Z—(CH2)p-A; R1 is selected from the group consisting of C1-C4 alkyl, C3-C6 cycloalkyl, CF3, hydroxy-substituted C1-C4 alkyl, hydroxy-substituted C3-C8 cycloalkyl, and NHR5, wherein R5 is C1-C3 alkyl or C3-C6 cycloalkyl; R2 is selected from the group consisting of: hydrogen, C1-C4 alkyl, C1-C4 alkyloxy, OCF3, CF3, hydroxyl, and halogen; R3 is selected from the group consisting of hydrogen, C1-C4 alkyl, C1-C4 alkyloxy, OCF3, CF3, hydroxyl, and halogen; R and R3 may be connected together to form an —O—(CH2)v bridge representing with the carbon atoms to which th
    Type: Grant
    Filed: January 12, 2007
    Date of Patent: July 29, 2014
    Assignees: McGill University, Universita Degli Studi di Parma, Universita Degli Studi di Milano, Universita Degli Studi di Urbino
    Inventors: Gabriella Gobbi, Marco Mor, Silvia Rivara, Franco Fraschini, Giorgio Tarzia, Annalida Bedini, Gilberto Spadoni, Valeria Lucini
  • Publication number: 20140117280
    Abstract: An oxygen absorber is provided that contains at least one of compounds each having a particular structure, and the oxygen absorber exhibits an oxygen absorbing capability without a metal contained, and is suitable for removing oxygen inside a packaging material packaging foods or the like.
    Type: Application
    Filed: May 16, 2012
    Publication date: May 1, 2014
    Applicant: MITSUBISHI GAS CHEMICAL COMPANY, INC.
    Inventors: Kentaro Ishii, Ryoji Otaki, Takafumi Oda, Shota Arakawa
  • Patent number: 8674135
    Abstract: One aspect of the present invention relates to ionic liquids comprising a pendant Bronsted-acidic group, e.g., a sulfonic acid group. Another aspect of the present invention relates to the use of an ionic liquid comprising a pendant Bronsted-acidic group to catalyze a Bronsted-acid-catalyzed chemical reaction. A third aspect of the present invention relates to ionic liquids comprising a pendant nucleophilic group, e.g., an amine. Still another aspect of the present invention relates to the use of an ionic liquid comprising a pendant nucleophilic group to catalyze a nucleophile-assisted chemical reaction. A fifth aspect of the present invention relates to the use of an ionic liquid comprising a pendant nucleophilic group to remove a gaseous impurity, e.g., carbon dioxide, from a gas, e.g., sour natural gas.
    Type: Grant
    Filed: February 26, 2010
    Date of Patent: March 18, 2014
    Assignee: University of South Alabama
    Inventor: James H. Davis, Jr.
  • Publication number: 20130331610
    Abstract: The invention provides novel halogenated pyrazolo[1,5-a]pyrimidines of formula (I) wherein R, R1, X and Y have different meanings, and pharmaceutically acceptable salts thereof. Compounds of formula (I) are useful for treating or preventing anxiety, epilepsy and sleep disorders including insomnia, and for inducing sedation-hypnosis, anesthesia, sleep and muscle relaxation. The invention also provides synthetic procedures for preparing said compounds and certain intermediates, as well as intermediates themselves.
    Type: Application
    Filed: August 13, 2013
    Publication date: December 12, 2013
    Applicant: Ferrer Internacional, S.A.
    Inventors: Luis Anglada, Albert Palomer, Antonio Guglietta
  • Patent number: 8492588
    Abstract: The present invention relates to benzyloxyanilide derivatives having the following structural formula: The compounds of the present invention are useful for the treatment and prevention of diseases and disorders which are affected by activation or modulation of potassium ion channels. One such condition is seizure disorders.
    Type: Grant
    Filed: May 29, 2012
    Date of Patent: July 23, 2013
    Assignee: Valeant Pharmaceuticals International
    Inventors: Jim Zhen Wu, Jean-Michel Vernier, Huanming Chen, Jianlan Song
  • Publication number: 20120232277
    Abstract: The present invention discloses processes for the preparation and isolation of [1,2,4]oxadiazo-3-yl derivatives of carboxylic acids. The derivatives are useful in the treatment of inflammatory diseases and conditions.
    Type: Application
    Filed: March 8, 2012
    Publication date: September 13, 2012
    Applicant: ABBOTT LABORATORIES
    Inventors: Kirill A. Lukin, Vimal Kishore, Thomas D. Gordon
  • Publication number: 20120214786
    Abstract: This invention relates to compounds of formula I their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions. A, M, W, R1, R2, R6, R7, R8 have meanings given in the description.
    Type: Application
    Filed: August 17, 2011
    Publication date: August 23, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Henning PRIEPKE, Henri DOODS, Raimund KUELZER, Roland PFAU, Dirk STENKAMP, Benjamin PELCMAN, Robert ROENN
  • Patent number: 8188314
    Abstract: The present invention relates to benzyloxyanilide derivatives having the following structural formula: The compounds of the present invention are useful for the treatment and prevention of diseases and disorders which are affected by activation or modulation of potassium ion channels. One such condition is seizure disorders.
    Type: Grant
    Filed: June 24, 2009
    Date of Patent: May 29, 2012
    Assignee: Valeant Pharmaceuticals International
    Inventors: Jim Zhen Wu, Jean-Michel Vernier, Huanming Chen, Jianlan Song
  • Patent number: 8178679
    Abstract: The present disclosure relates to 4-(2-amino-1-hydroxyethyl)phenol derivatives of formula (I) as well as pharmaceutical compositions comprising them, and their use in therapy as agonists of the ?2 adrenergic receptor.
    Type: Grant
    Filed: November 10, 2008
    Date of Patent: May 15, 2012
    Assignee: Almirall, S.A.
    Inventors: Victor Giulio Matassa, Carlos Puig Duran, Maria Prat Quiñones, Laia Sole Feu, Oriol Llera Soldevila
  • Patent number: 8110706
    Abstract: A method of preparation of a highly pure salt of R,R-formoterol L-tartrate is disclosed. The process provides the most thermodynamically stable polymorph by recrystallization of a novel polymorph.
    Type: Grant
    Filed: April 26, 2010
    Date of Patent: February 7, 2012
    Assignee: Sunovion Pharmaceuticals Inc.
    Inventors: Gerald J. Tanoury, Chris H. Senanayake, Donald W. Kessler
  • Publication number: 20110294830
    Abstract: The present invention provides a nitrogen-containing compound represented by formula (I1) (in formula (I1), R0 represents a nitro group or the like, Z represents an optionally substituted aryl group or the like, R3 represents a hydrogen atom or the like, Y represents a nitro group or the like, n represents an integer of 0 to 3, D represents an optionally substituted 5-membered to 8-membered hydrocarbon ring group or heterocyclic group having or not having a substituent other than substituent X, X represents a group represented by formula (II-1) (in formula (II-1), R1 and R2 respectively and independently represent a hydrogen atom or the like), A represents a carbon atom or the like, n1 represents an integer of 0 to 2) or a salt thereof, and an insecticide, miticide, sanitary insect pest control agent, or harmful organism control agent including as an active ingredient thereof the nitrogen-containing compound or the salt thereof.
    Type: Application
    Filed: February 5, 2010
    Publication date: December 1, 2011
    Applicant: Nippon Soda Co., Ltd.
    Inventors: Jyun Iwata, Masahiro Kawaguchi, Akiko Mizui
  • Patent number: 7964753
    Abstract: A method of preparation of a highly pure salt of R,R-formoterol L-tartrate is disclosed. The process provides the most thermodynamically stable polymorph by recrystallization of a novel polymorph.
    Type: Grant
    Filed: June 7, 2010
    Date of Patent: June 21, 2011
    Assignee: Sunovion Pharmaceuticals Inc.
    Inventors: Gerald J. Tanoury, Chris H. Senanayake, Donald W. Kessler
  • Publication number: 20100324000
    Abstract: The present disclosure relates to 4-(2-amino-1-hydroxyethyl)phenol derivatives of formula (I) as well as pharmaceutical compositions comprising them, and their use in therapy as agonists of the ?2 adrenergic receptor.
    Type: Application
    Filed: November 10, 2008
    Publication date: December 23, 2010
    Inventors: Victor Giulio Matassa, Carlos Puig Duran, Maria Prat Quiñones, Laia Sole Fue, Oriol Llera Soldevila
  • Publication number: 20100298328
    Abstract: 1-Heterocyclylamino-2-hydroxy-3-amino-?-arylalkanes of formula (I) and the salts thereof have renin-inhibiting properties and can be used as antihypertensive, medicinally active ingredients.
    Type: Application
    Filed: March 30, 2007
    Publication date: November 25, 2010
    Inventors: John J. Baldwin, David A. Claremon, Lawrence W. Dillard, Alexey V. Ishchenko, Jing Yuan, Zhenrong Xu, Gerard McGeehan, Wenguang Zeng
  • Publication number: 20100267836
    Abstract: Novel melatonin ligands of Formula I: or pharmaceutically acceptable salts thereof wherein: n is 1 or 2; m is 0, 1 or 2; p is 0, 1, 2, 3, 4, 5, 6, 7 or 8; v is 2 or 3; A is aryl or heteroaryl; Z is O, S or NR8; Y is selected from the group consisting of hydrogen, aryl, heteroaryl, C1-C6 alkyl, C3-C6 cycloalkyl, and R is selected from the group consisting of hydrogen, hydroxyl, —OCF3, CF3, C1-C8 alkyl, C1-C8 alkyloxy, C1-C8 alkylthio, halogen and —Z—(CH2)p-A; R1 is selected from the group consisting of C1-C4 alkyl, C3-C6 cycloalkyl, CF3, hydroxy-substituted C1-C4 alkyl, hydroxy-substituted C3-C8 cycloalkyl, and NHR5, wherein R5 is C1-C3 alkyl or C3-C6 cycloalkyl; R2 is selected from the group consisting of: hydrogen, C1-C4 alkyl, C1-C4 alkyloxy, OCF3, CF3, hydroxyl, and halogen; R3 is selected from the group consisting of hydrogen, C1-C4 alkyl, C1-C4 alkyloxy, OCF3, CF3, hydroxyl, and halogen; R and R3 may be connected together to form an —O—(CH2)v bridge representing with the carbon atoms to which the
    Type: Application
    Filed: January 12, 2007
    Publication date: October 21, 2010
    Applicants: UNIVERSITA DEGLI STUDI DI MILANO, UNIVERSITA DEGLI STUDI DI URBINO, MCGILL UNIVERSITY, UNIVERSITA DEGLI STUDI DI PARMA
    Inventors: Gabriella Gobbi, Marco Mor, Silvia Rivara, Franco Fraschini, Giorgio Tarzia, Annalida Bedini, Gilberto Spadoni, Valeria Lucini
  • Publication number: 20100267697
    Abstract: The present teachings provide compounds of Formula (I) and pharmaceutically acceptable salts, hydrates, and esters thereof, wherein Ar, R1, R2, R3, p, and X are defined herein. The present teachings also provide processes for producing said compounds and their pharmaceutically acceptable salts, hydrates and esters, and methods of treating a pathological condition or disorder, or alleviating a symptom thereof, using said compounds including their pharmaceutically acceptable salts, hydrates and esters. The compounds can be useful in modulating ion channel activity including treating a variety of conditions associated with the abnormal modulation of one or more voltage-gated calcium channels.
    Type: Application
    Filed: December 11, 2007
    Publication date: October 21, 2010
    Applicant: Wyeth
    Inventors: Vincent P. Galullo, Robert Zelle, Danielle Soenen, Christopher Todd Baker, Paul Will, Hormoz Mazdiyasni, Jinsong Guo, Andrew Fensome, Jeffrey Curtis Kern, William Jay Moore, Edward George Melenski, Justin Kaplan
  • Publication number: 20100204336
    Abstract: A method of preparation of a highly pure salt of R,R-formoterol L-tartrate is disclosed. The process provides the most thermodynamically stable polymorph by recrystallization of a novel polymorph.
    Type: Application
    Filed: April 26, 2010
    Publication date: August 12, 2010
    Applicant: SEPRACOR INC.
    Inventors: Gerald J. Tanoury, Chris H. Senanayake, Donald W. Kessler
  • Patent number: 7754920
    Abstract: This invention relates to an improved method for crystallizing 5-acetamido-N,N?-bis(2,3-dihydroxypropyl)-2,4,6-triiodoisophthalamide (“Compound A”), an intermediate in the industrial preparation of non-ionic X-ray contrast agents. In particular, the present invention provides an industrial process for crystallization of Compound A by evaporating methanol and water from the mother liquor after an initial crystallization of Compound A following the acetylation reaction. Specifically, the mother liquor is maintained at more than about 75% (v/v) of water and less than about 25% (v/v) of alcoholic solvent.
    Type: Grant
    Filed: November 18, 2009
    Date of Patent: July 13, 2010
    Assignee: GE HealthCare AS
    Inventors: Lars Terje Holmaas, Kristin Rypestol
  • Publication number: 20100145056
    Abstract: Disclosed are compounds of the formula: where variables Z, X, R15, R2, R3, and Rc are defined herein. Compounds disclosed herein are inhibitors of the beta-secretase enzyme and are therefore useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal.
    Type: Application
    Filed: November 23, 2009
    Publication date: June 10, 2010
    Inventors: Varghese John, Michel Maillard, James P. Beck, Eric T. Baldwin, Robert Hughes, Shon R. Pulley, Ruth T. TenBrink
  • Publication number: 20100144741
    Abstract: The invention relates to novel cyclic compounds of the formula (I), in free base form or in acid addition salt form, to their preparation, to their use as medicaments and to medicaments comprising them.
    Type: Application
    Filed: November 22, 2007
    Publication date: June 10, 2010
    Inventors: Mathias Frederiksen, Rainer Martin Luond, Clive McCarthy, Henrik Moebitz, Jean-Michel Rondeau, Bernard Lucien Roy, Heinrich Rueeger
  • Patent number: 7732641
    Abstract: A method of preparation of a highly pure salt of R,R-formoterol L-tartrate is disclosed. The process provides the most thermodynamically stable polymorph by recrystallization of a novel polymorph.
    Type: Grant
    Filed: December 5, 2008
    Date of Patent: June 8, 2010
    Assignee: Sepracor Inc.
    Inventors: Gerald J. Tanoury, Chris H. Senanayake, Donald W. Kessler
  • Publication number: 20090312380
    Abstract: This invention relates to active pharmaceutical ingredients (APIs) with specific water surface areas, to pharmaceutical compositions comprising said APIs, to processes for preparing such compositions, and to methods for determining the water surface areas of substances such as APIs and other particles.
    Type: Application
    Filed: August 31, 2007
    Publication date: December 17, 2009
    Inventor: Axel Becker
  • Patent number: 7601870
    Abstract: The present invention relates to aniline derivatives of the general formula I or salts thereof, described therein, and their use.
    Type: Grant
    Filed: December 20, 2005
    Date of Patent: October 13, 2009
    Assignee: H. Lundbeck A/S
    Inventors: Christian Wenzel Tornøe, Mario Rottländer, Daniel Rodriguez Greve, Nikolay Khanzhin, Andreas Ritzén, William Patrick Watson
  • Publication number: 20090247751
    Abstract: A process for the preparation of N-[3-[3-(dimethylamino)-1-oxo-2-propenyl]phenyl]-N-ethyl acetamide of formula II, comprising reacting a compound N-[3-[3-(dimethylamino)-1-oxo-2-propenyl]phenyl]acetamide of formula III, with an ethylating agent in the presence of a strong alkali metal hydroxide and a phase transfer catalyst in a polar-aprotic solvent, and a process for preparation of Zaleplon, which is substantially free of impurities using the said compound of formula II.
    Type: Application
    Filed: February 13, 2007
    Publication date: October 1, 2009
    Applicant: PIRAMAL HEALTHCARE LIMITED
    Inventors: Vilas Vasant Pandit, Rajesh Vinodrai Naik, Abhay Atmaram Upare, Rajmohan Shivraj Ubale
  • Patent number: 7544717
    Abstract: Disclosed are compounds of the formula: where variables Q, Z, X, R15, R2, R3, and Rc are defined herein. Compounds disclosed herein are inhibitors of the beta-secretase enzyme and are therefore useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal.
    Type: Grant
    Filed: March 25, 2005
    Date of Patent: June 9, 2009
    Assignee: Elan Pharmaceuticals, Inc.
    Inventors: Roy Hom, John Tucker, Varghese John, Neerav Shah
  • Patent number: 7479572
    Abstract: A method of preparation of a highly pure salt of R,R-formoterol L-tartrate is disclosed. The process provides the most thermodynamically stable polymorph by recrystallization of a novel polymorph.
    Type: Grant
    Filed: January 14, 2008
    Date of Patent: January 20, 2009
    Assignee: Sepracor Inc.
    Inventors: Gerald J. Tanoury, Chris H. Senanayaka, Donald W. Kessler
  • Patent number: 7378448
    Abstract: A compound of the formula (I) wherein the variables X1, X2, B, D, R1 to R7 including R3?, p, y, q, and z, are as defined or a pharmaceutically acceptable salt, solvate, enantiomer, racemate, diastereomer or mixtures thereof, useful for the treatment, prevention or amelioration of obesity and Related Diseases is disclosed
    Type: Grant
    Filed: March 2, 2005
    Date of Patent: May 27, 2008
    Assignee: Eli Lilly and Company
    Inventors: Charles Howard Mitch, Steven James Quimby, Miles Goodman Siegel
  • Patent number: 7342132
    Abstract: A method of preparation of a highly pure salt of R,R-formoterol L-tartrate is disclosed. The process provides the most thermodynamically stable polymorph by recrystallization of a novel polymorph.
    Type: Grant
    Filed: August 4, 2006
    Date of Patent: March 11, 2008
    Assignee: Sepracor Inc.
    Inventors: Gerald J. Tanoury, Chris H. Senanayake, Donald W. Kessler
  • Publication number: 20080045534
    Abstract: This invention provides compounds of formula I where X?O or S; Y is O or S; q=1 or 0; and other substituents are defined herein. The invention also provides pharmaceutical compositions comprising compounds of formula I. Such compounds are potassium channel modulators.
    Type: Application
    Filed: August 16, 2007
    Publication date: February 21, 2008
    Applicant: Valeant Pharmaceuticals North America
    Inventors: Jean-Michel Vernier, Samedy Ouk, Martha Alicia De La Rosa, David Abraham Paisner
  • Patent number: 7211695
    Abstract: Disclosed are multibinding compounds which are ?2-adrenergic receptor agonists and are useful in the treatment and prevention of respiratory diseases such as asthma, bronchitis. They are also useful in the treatment of nervous system injury and premature labor.
    Type: Grant
    Filed: April 10, 2006
    Date of Patent: May 1, 2007
    Assignee: Theravance, Inc.
    Inventors: Edmund J. Moran, Seok-Ki Choi
  • Patent number: 7145036
    Abstract: A method of preparation of a highly pure salt of R,R-formoterol L-tartrate is disclosed. The process provides the most thermodynamically stable polymorph by recrystallization of a novel polymorph.
    Type: Grant
    Filed: February 7, 2005
    Date of Patent: December 5, 2006
    Assignee: Sepracor Inc.
    Inventors: Gerald J. Tanoury, Chris H. Senanayake, Donald W. Kessler
  • Patent number: 7105701
    Abstract: Disclosed are multibinding compounds which are ?2-adrenergic receptor agonists and are useful in the treatment and prevention of respiratory diseases such as asthma, bronchitis. They are also useful in the treatment of nervous system injury and premature labor.
    Type: Grant
    Filed: May 10, 2005
    Date of Patent: September 12, 2006
    Assignee: Theravance, Inc.
    Inventors: Edmund J. Moran, Seok-Ki Choi
  • Patent number: 6916956
    Abstract: A compound of the formula [I] wherein R1 is optionally substituted aryl group or optionally substituted heteroaryl group; R2 is optionally substituted C1-6 alkyl group, C3-7 cycloalkyl group and the like; R3 is hydrogen atom, C1-6 alkyl group, hydroxyl group and the like; R4 is hydrogen atom, C1-6 alkyl group and the like; R5 and R6 are each C1-6 alkyl group and the like; R7 is optionally substituted aryl group or optionally substituted heteroaryl group; X1, X2 and X3 are each C1-6 alkylene group and the like; and X4 and X5 are each a single bond, methylene group and the like, a salt thereof, a solvate thereof or a prodrug thereof, and a pharmaceutical composition containing the compound, particularly a calcium receptor antagonist and a therapeutic agent for osteoporosis, are provided.
    Type: Grant
    Filed: August 10, 2001
    Date of Patent: July 12, 2005
    Assignee: Japan Tobacco, Inc.
    Inventors: Yuko Shinagawa, Takeo Katsushima, Takashi Nakagawa
  • Patent number: 6720453
    Abstract: A method of preparation of a highly pure salt of R,R-formoterol L-tartrate is disclosed. The process provides the most thermodynamically stable polymorph by recrystallization of a novel polymorph.
    Type: Grant
    Filed: September 10, 2002
    Date of Patent: April 13, 2004
    Assignee: Sepracor Inc.
    Inventors: Gerald J. Tanoury, Chris H. Senanayake, Donald W Kessler
  • Patent number: 6635650
    Abstract: The invention relates to compounds of formula (I): A-G1-Cy-G2-Cy-G3-B  (I) wherein: A represents NR1C(Q)R2, C(Q)NR2R3 or NR1C(Q)NR2R3, B represents NR1C(Q)R2, C(Q)NR2R3, NR1C(Q)NR2R3, C(Q)OR1, NR1C(Q)OR2 or NR2R3, G1 and G3 represent an optionally substituted alkylene chain, Cy represents a ring structure G2 represents a chain and medicinal products containing the same which are useful in treating or in preventing melatoninergic disorders.
    Type: Grant
    Filed: August 8, 2001
    Date of Patent: October 21, 2003
    Assignee: Les Laboratoires Servier
    Inventors: Daniel Lesieur, Said Yous, Carole Descamps-Francois, François Lefoulon, Gérald Guillaumet, Marie-Claude Viaud, Caroline Bennejean, Philippe Delagrange, Pierre Renard
  • Patent number: 6576793
    Abstract: Disclosed are multibinding compounds which are &bgr;2 adrenergic receptor agonists and are useful in the treatment and prevention of respiratory diseases such as asthma and bronchitis. They are also useful in the treatment of nervous system injury and premature labor.
    Type: Grant
    Filed: August 14, 2000
    Date of Patent: June 10, 2003
    Assignee: Theravance, Inc.
    Inventors: Edmund J. Moran, John H. Griffin, Seok-Ki Choi
  • Patent number: 6537524
    Abstract: A medicament containing, separately or together, (A) formoterol or a pharmaceutically acceptable salt thereof or a solvate of formoterol or said salt and (B) a tiotropium salt of a pharmaceutically acceptable acid, for simultaneous, sequential or separate administration in the treatment of an inflammatory or obstructive airways disease.
    Type: Grant
    Filed: August 8, 2001
    Date of Patent: March 25, 2003
    Assignee: Novartis AG
    Inventors: Ian Francis Hassan, Jeremy Guy Clarke, Bernard Cuenoud
  • Patent number: 6472563
    Abstract: A method of preparation of a highly pure salt of R,R-formoterol L-tartrate is disclosed. The process provides the most thermodynamically stable polymorph by recrystallization of a novel polymorph.
    Type: Grant
    Filed: November 9, 2001
    Date of Patent: October 29, 2002
    Assignee: Sepracor Inc.
    Inventors: Gerald J. Tanoury, Chris H. Senanayake, Donald W Kessler
  • Patent number: 6472393
    Abstract: Compounds having the structure shown below wherein A, B, N1, N2, X, Y, Q, R2, R5 and R6 are as defined herein are useful to inhibit serine protease enzymes, such as TF/factor VIIa factor Xa, thrombin and kallikrein. These compounds may be used in methods of preventing and/or treating clotting disorders.
    Type: Grant
    Filed: March 21, 2000
    Date of Patent: October 29, 2002
    Assignee: Genentech, Inc.
    Inventors: Ignacio Aliagas-Martin, Dean R. Artis, Michael S. Dina, John A. Flygare, Richard A. Goldsmith, Regina A. Munroe, Alan G. Olivero, Richard Pastor, Thomas E. Rawson, Kirk D. Robarge, Daniel P. Sutherlin, Kenneth J. Weese, Aihe Zhou, Yan Zhu
  • Patent number: 6423714
    Abstract: The compounds of formula I are useful in treating gastrointestinal disorders associated with antagonizing the motilin receptor. The compounds compete with erythromycin and motilin for the motilin receptor. In addition the compounds are antagonists of the contractile smooth muscle response to those ligands.
    Type: Grant
    Filed: March 9, 2001
    Date of Patent: July 23, 2002
    Assignee: Ortho McNeil-Pharmaceutical, Inc..
    Inventors: Robert H. Chen, Min A. Xiang
  • Patent number: 6319930
    Abstract: The invention relates to compounds of formula (I): A—G1—Cy—G2—Cy—G3—B  (I) wherein: A represents NR1C(Q)R2, C(Q)NR2R3 or NR1C(Q)NR2R3, B represents NR1C(Q)R2, C(Q)NR2R3, NR1C(Q)NR2R3, C(Q)OR1, NR1C(Q)OR2 or NR2R3, G1 and G3 represent an optionally substituted alkylene chain, Cy represents a ring structure and G2 represents a chain and medicinal products containing the same which are useful in treating or in preventing melatoninergic disorders.
    Type: Grant
    Filed: March 24, 2000
    Date of Patent: November 20, 2001
    Assignee: Adir et Compagnie
    Inventors: Daniel Lesieur, Said Yous, Carole Descamps-Francois, François Lefoulon, Gérald Guillaumet, Marie-Claude Viaud, Caroline Bennejean, Philippe Delagrange, Pierre Renard
  • Patent number: 6268533
    Abstract: A method is disclosed for the preparation of optically pure isomers of formoterol by the reaction of an optically pure 4-benzyloxy-3-formamidostyrene oxide with an optically pure 4-methoxy-&agr;-methyl-N-(phenylmethyl)benzeneethanamine followed by debenzylation. Useful intermediates in the process are also disclosed, as are the novel L-tartrate salt of R,R-formoterol and pharmaceutical compositions thereof.
    Type: Grant
    Filed: January 27, 2000
    Date of Patent: July 31, 2001
    Assignee: Sepracor Inc.
    Inventors: Yun Gao, Robert Hett, Kevin Q. Fang, Stephen A. Wald, Chris Hugh Senanayake
  • Patent number: 6265445
    Abstract: The present invention relates to novel, antiarrhythmically active phenoxyalkylamine derivatives possessing a double point of attack. More particularly, the present invention relates to new phenoxyalkylamine derivatives of the formula (1) wherein R1 and R2, independently from each other, mean hydrogen, halogen or C1-4 alkyl group; R3, R4 and R5, independently from each other, stand for hydrogen or C1-4 alkyl group; R6 represents hydrogen, C1-4 alkyl or benzyl group; R7 means nitro group or amino group optionally monosubstituted by C1-4 alkyl, benzoyl, C1-4 alkylcarbonyl, C1-4 alkylsulfonyl, C1-4 alkylcarbamoyl or C1-4 alkylthiocarbamoyl group; both n and m are 0 or 1, with the proviso that R2 is different from hydrogen, when R1 is hydrogen, as well as stereoisomers or mixtures of stereoisomers thereof, acid addition salts thereof and hydrates, prodrugs and metabolites of all these compounds.
    Type: Grant
    Filed: July 28, 2000
    Date of Patent: July 24, 2001
    Assignees: Gyogyszerkutato Intezet Kft, Szent-Gyorgyi Albert Orvostudomanyi Egyetem
    Inventors: Gyula Papp, András Varró, Péter Mátyus, Ildikó Varga, Tivadar Rettegi, Alice Druga, Antal Simay, Imre Moravcsik, Pál Berzsenyi, Daniella Barlocco, Giorgio Cignarella, Márta Pátfalusi
  • Patent number: 6258852
    Abstract: Disclosed are methods for treating or preventing inflammatory bowel disease (IBD) using aryl nitrone compounds. Pharmaceutical compositions containing aryl nitrone compounds which are useful for the treatment or prophylaxis of IBD are also disclosed.
    Type: Grant
    Filed: May 8, 2000
    Date of Patent: July 10, 2001
    Assignee: Centaur Pharmaceuticals, Inc.
    Inventors: William D. Flitter, William A. Garland, Beverly Greenwood Van-Meerveld, Ian Irwin
  • Patent number: 6232498
    Abstract: There are described processes for the preparation of a compound of formula I and novel intermediates in the preparative process.
    Type: Grant
    Filed: October 1, 1999
    Date of Patent: May 15, 2001
    Assignee: Astra Zeneca UK Limited
    Inventor: Christopher Goodwin
  • Patent number: 6194614
    Abstract: There are described processes for the preparation of a compound of formula I and novel intermediates in the preparative process.
    Type: Grant
    Filed: October 1, 1999
    Date of Patent: February 27, 2001
    Assignee: AstraZeneca UK Limited
    Inventor: Christopher Goodwin
  • Patent number: 6133315
    Abstract: Amidino and benzamidino compounds, including compounds of the formula: ##STR1## wherein R.sup.1 -R.sup.4, R.sup.6 -R.sup.9, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit a number of proteolytic enzymes are described. Also described are methods for preparing the compounds of Formula I.
    Type: Grant
    Filed: March 16, 1999
    Date of Patent: October 17, 2000
    Assignee: 3-Dimensional Pharmaceuticals, Inc.
    Inventors: Tianbao Lu, Bruce E. Tomczuk, Carl R. Illig, Richard M. Soll
  • Patent number: 6028112
    Abstract: There is provided novel spirocyclopropyl fluorene derivatives having the general Formula I ##STR1## wherein R, R.sup.1 and X are as defined herein which are useful as melatonergic agents.
    Type: Grant
    Filed: July 31, 1998
    Date of Patent: February 22, 2000
    Assignee: Bristol-Myers Squibb Company
    Inventors: Karen L. Leboulluec, Katherine S. Takaki
  • Patent number: 6018069
    Abstract: A purified acid addition salt of a (2S, 3S, 5S)-2,5-diamino-1,6-diphenyl-3-hydroxyhexane, e.g., (2S, 3S, 5S)-2-tert-butoxycarbonylamino-3-hydroxy-5-amino-1,6-diphenylhexane, is obtained from its mixture, in an arbitrary ratio, with its (2S, 3S, 5R) stereoisomer in the presence of an inorganic or organic acid. The desired (2S, 3S, 5S) acid addition salt may be recovered from the mixture by, for example, recrystallization. These purified acid addition salts are useful as intermediates in the synthesis of medicines such as retrovirus protease inhibitors including human immunodeficiency virus (HIV) protease inhibitors.
    Type: Grant
    Filed: May 26, 1999
    Date of Patent: January 25, 2000
    Assignee: Daicel Chemical Industries, Ltd.
    Inventors: Yoshiyuki Murai, Masahiro Nishikawa, Yoichiro Ueda, Ichiro Takase