Acyclic Nitrogen Double Or Triple Bonded To Carbon Which Is Attached Directly Or Indirectly To The Isoquinoline Ring System By Nonionic Bonding Patents (Class 546/145)
  • Publication number: 20150065538
    Abstract: Compounds of formula (I) wherein R1, R2, R3, and Y are defined in the description are TRPA1 antagonists. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.
    Type: Application
    Filed: November 4, 2014
    Publication date: March 5, 2015
    Inventors: Richard J. Perner, Michael E. Kort, Stanley DiDomenico, Jun Chen, Anil Vasudevan
  • Publication number: 20140323482
    Abstract: The present invention provides a compound of Formula I (The formula should be inserted here) as described herein or a pharmaceutically acceptable salt or solvate thereof. The representative compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same.
    Type: Application
    Filed: December 17, 2012
    Publication date: October 30, 2014
    Inventors: Yao Ma, Manami Shizuka, Timothy J. Guzi, Yuan Liu, Yuan Tian, Brian R. Lahue, Craig R. Gibeau, Gerald W. Shipps, JR., Yaolin Wang, Stephane L. Bogen, Latha G. Nair, Weidong Pan, Mark A. McCoy, Matthew E. Voss, Margarita Kirova-Snover, W. Bent Clayton
  • Publication number: 20140274960
    Abstract: The present invention provides compounds of Formula (I) or stereoisomers, pharmaceutically acceptable salts thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of factor XIa and/or plasma kallikrein which may be used as medicaments.
    Type: Application
    Filed: October 12, 2012
    Publication date: September 18, 2014
    Inventors: Michael J. Orwat, Donald J.P. Pinto, Leon M. Smith, II, Shefali Srivastava
  • Publication number: 20140228576
    Abstract: Provided are an efficient method for producing 3,4-dihydroisoquinoline derivatives and useful production intermediates thereof. Provided is a method for producing 3,4-dihydroisoquinoline derivatives represented by general formula (1), comprising converting a compound represented by general formula (3) in the presence of acid after reacting with an aniline derivative, or converting a compound represented by general formula (3) by reacting with an aniline derivative in the presence of an acid.
    Type: Application
    Filed: September 28, 2012
    Publication date: August 14, 2014
    Applicant: MITSUI CHEMICALS AGRO, INC.
    Inventors: Hideki Umetani, Nobuhiro Kondo, Fumie Kajino, Munetsugu Morimoto
  • Publication number: 20140193518
    Abstract: The invention relates to kinase inhibitor compounds and methods of identifying and using them. The invention further relates to pharmaceutical compositions and methods for treating disorders, especially cancer.
    Type: Application
    Filed: December 28, 2012
    Publication date: July 10, 2014
    Applicant: UNIVERSITY OF FLORIDA RESEARCH FOUNDATION, INC.
    Inventor: UNIVERSITY OF FLORIDA RESEARCH FOUNDATION, INC.
  • Patent number: 8741923
    Abstract: The invention provides compounds of Formula (I) for the treatment of multiple sclerosis and other diseases.
    Type: Grant
    Filed: December 15, 2009
    Date of Patent: June 3, 2014
    Assignee: Merck Serono SA
    Inventors: Mathilde Muzerelle, Anna Quattropani, Cyril Montagne, Jérôme Dorbais
  • Publication number: 20140135327
    Abstract: This invention relates to the discovery of novel compounds, or pharmaceutically acceptable salts thereof, which possess HDAC inhibitory activity. In particular, the compounds of the invention demonstrate selectivity towards Class I HDAC enzymes, and are accordingly expected to be useful for their anti-proliferative activity and in methods of treatment of the human or animal body, for example in preventing or inhibiting tumour growth and metastasis in cancers. The invention also relates to processes for the manufacture of the compounds defined herein, or pharmaceutically acceptable salts thereof, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments for use in the production of an anti-proliferative effect in a warm-blooded animal such as man.
    Type: Application
    Filed: July 6, 2012
    Publication date: May 15, 2014
    Applicant: CANCER RESEARCH TECHNOLOGY LIMITED
    Inventors: Ronald Ernest Grigg, Martyn Inman, Graham Packham
  • Publication number: 20130317010
    Abstract: To provide an excellent agent for preventing or treating dementia and schizophrenia based on serotonin 5-HT5A receptor regulating action, it was found that a tetrahydroisoquinoline derivative characterized by a structure in which an acylguanidino group binds to a N atom of a tetrahydroisoquinoline ring or the like, and a cyclic group binds to an unsaturated ring has a potent 5-HT5A receptor regulating action and an excellent pharmacological action based on the regulating action and also discovered that the tetrahydroisoquinoline derivative is useful as an agent for treating or preventing dementia, schizophrenia, and the like, whereby the present invention has been completed.
    Type: Application
    Filed: August 1, 2013
    Publication date: November 28, 2013
    Applicant: Astellas Pharma Inc
    Inventors: Wataru HAMAGUCHI, Isao KINOYAMA, Yohei KOGANEMARU, Takehiro MIYAZAKI, Osamu KANEKO, Ryuichi SEKIOKA, Takuya WASHIO
  • Publication number: 20130203802
    Abstract: A compound of Formula (I) or a pharmaceutically acceptable salt thereof: Wherein: Het is a 5 to 10-membered heteroaromatic ring; Either X is N and Y is CR5; or X is C and Y is S; Z is selected from N and CH; R1 is selected from H and C1-2alkyl; R2 is selected from H, C1-2alkyl, OH, —CH2OH and C1-2alkoxy; Each R3 is independently selected from OH, C1-3alkyl, F, Cl, Br, NH2, and C1-3alkoxy; R4 is selected from C1-3alkyl and haloC1-3alkyl; R5 is selected from H, C1-3alkyl and haloC1-3alkyl; R6 and R7 are either i) each independently selected from H, C1-3alkyl and C1-3alkoxy; or ii) R6 and R7 together with the ring to which they are attached form a 9-membered bicyclic ring; p is 0-3; and RA is selected from H and C1-3alkyl, compositions containing them, their use in therapy, for example in the treatment of tuberculosis, and methods for the preparation of such compounds, are provided.
    Type: Application
    Filed: October 11, 2011
    Publication date: August 8, 2013
    Applicant: GLAXO GROUP LIMITED
    Inventors: Julia Castro Pichel, Raquel Fernandez Menendez, Esther Pilar Fernandez Velando, Silvia Gonzalez Del Valle, Araceli Mallo-Rubio
  • Publication number: 20130143916
    Abstract: A method for producing libraries of structurally and stereochemically diverse molecules that can be screened for biological or chemical activity. A library of 91 heterocyclic compounds composed of 16 distinct scaffolds was synthesized through a sequence of phosphine-catalyzed ring-forming reactions, Tebbe reactions, Diels-Alder reactions, and, in some cases, hydrolysis to illustrate the methods. Three compounds inhibiting migration of human breast cancer cells are identified from the library.
    Type: Application
    Filed: November 9, 2012
    Publication date: June 6, 2013
    Applicants: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: THE REGENTS OF THE UNIVERSITY OF CALIF, Gabriel Fenteany
  • Publication number: 20130059873
    Abstract: The present invention relates to compounds which inhibit dipeptidyl peptidase IV (DPP-IV) and are useful for the prevention or treatment of diabetes, especially type II diabetes, as well as hyperglycemia, Syndrome X, hyperinsulinemia, obesity, atherosclerosis, and various immunomodulatory diseases.
    Type: Application
    Filed: April 3, 2012
    Publication date: March 7, 2013
    Inventors: David J. Madar, Stevan W. Djuric, Melissa J. Michmerhuizen, Hana A. Kopecka, Xiaofeng Li, Kenton L. Longenecker, Zhonghua Pei, Daisy Pireh, Hing L. Sham, Kent D. Stewart, Bruce G. Szczepankiewicz, Paul E. Wiedeman, Hong Yong
  • Patent number: 8362020
    Abstract: The present disclosure is generally directed to antiviral compounds, and more specifically directed to compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such compounds, and methods for inhibiting the function of the NS5A protein.
    Type: Grant
    Filed: December 21, 2010
    Date of Patent: January 29, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventors: Omar D. Lopez, Denis R. St. Laurent, Jason Goodrich, Jeffrey Lee Romine, Michael Serrano-Wu, Fukang Yang, Ramesh Kakarla, Xuejie Yang, Yuping Qiu, Lawrence B. Snyder
  • Patent number: 8273767
    Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).
    Type: Grant
    Filed: August 3, 2010
    Date of Patent: September 25, 2012
    Assignee: Abbott Laboratories
    Inventors: Robert J. Altenbach, Lawrence A. Black, Sou-Jen Chang, Marlon D. Cowart, Ramin Faghih, Gregory A. Gfesser, Yi-Yin Ku, Huaqing Liu, Kirill A. Lukin, Diana L. Nersesian, Yu-ming Pu, Padam N. Sharma, Youssef L. Bennani, Michael P. Curtis
  • Publication number: 20120232019
    Abstract: The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides for diagnosis of an LFA-1 mediated disease and administration of a LFA-1 antagonist, after the patient is diagnosed with a LFA-1 mediated disease. In some embodiments, the LFA-1 mediated diseases treated are dry eye disorders. Also provided herein are methods for identifying compounds which are LFA-1 antagonists.
    Type: Application
    Filed: February 16, 2012
    Publication date: September 13, 2012
    Applicant: SARcode Bioscience Inc.
    Inventors: Thomas Gadek, John Burnier, Johan Oslob, Wang Shen, Kenneth Barr, Min Zhong
  • Publication number: 20120101083
    Abstract: The present invention relates to novel compounds of formula (I) having S1P1 agonist activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.
    Type: Application
    Filed: June 17, 2010
    Publication date: April 26, 2012
    Applicant: GLAXO GROUP LIMITED
    Inventors: James Matthew Bailey, Rino Antonio Bit, Emmanuel Hubert Demont, Lee Andrew Harrison, Katherine Louise Jones, Christian Alan Paul Smethurst, Jason Witherington
  • Publication number: 20120094979
    Abstract: Thiazole or thiadizaloe derivatives of formula (I) or pharmaceutical salts thereof having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their uses in the treatment of various disorders mediated by S1P1 receptor are disclosed.
    Type: Application
    Filed: June 17, 2010
    Publication date: April 19, 2012
    Applicant: Glaxo Wellcome House
    Inventors: James Matthew Bailey, Emmanuel Hubert Demont, Xichen Lin, Feng Ren, Christian Alan Paul Smethurst
  • Patent number: 8158796
    Abstract: The present invention is directed to practical high-yielding synthetic processes to prepare compounds of general Formula III, IV, V, VII, VIII, IX, X, XII, XIV, and XV. Such compounds are useful as final products or can be used as intermediates and be further modified to prepare other desired products such as rho-kinase inhibitors. The present invention is also directed to certain novel compounds and/or novel solid forms of certain compounds.
    Type: Grant
    Filed: May 21, 2009
    Date of Patent: April 17, 2012
    Assignee: Inspire Pharmaceuticals, Inc.
    Inventors: Jin She, Jonathan Bryan deCamp, Paul S. Watson, David J. Slade
  • Publication number: 20120077793
    Abstract: The present invention is directed to therapeutic compounds which have activity as agonists of GPR119 and are useful for the treatment of metabolic disorders including type II diabetes.
    Type: Application
    Filed: March 12, 2010
    Publication date: March 29, 2012
    Applicant: PROSIDION LIMITED
    Inventors: Oscar Barba, Peter Timothy Fry, Matthew Colin Thor Fyfe, William Gattrell, Revathy Perpetua Jeevaratnam, Thomas Martin Krulle, Martin James Procter, Colin Peter Sambrook-Smith, Karen Lesley Schofield, Donald Smyth, Alan John William Stewart, David French Stonehouse, Simon Andrew Swain
  • Publication number: 20110306621
    Abstract: An object of the present invention is to provide an excellent agent for treating or preventing dementia, schizophrenia based on a serotonin 5-HT5A receptor modulating action. It was confirmed that acylguanidine derivatives, which has the characteristic structure in which the guanidine is bonded to one ring of a naphthalene via a carbonyl group and a cyclic group is bonded to the other ring thereof, exhibit potent 5-HT5A receptor modulating action and excellent pharmacological action based on the action. The present invention is useful as an excellent agent for treating or preventing dementia, schizophrenia, bipolar disorder or attention deficit hyperactivity disorder.
    Type: Application
    Filed: February 8, 2010
    Publication date: December 15, 2011
    Inventors: Isao Kinoyama, Takehiro Miyazaki, Yohei Koganemaru, Nobuyuki Shiraishi, Yuichiro Kawamoto, Takuya Washio
  • Publication number: 20110230518
    Abstract: The invention provides compounds of Formula (I) for the treatment of multiple sclerosis and other diseases.
    Type: Application
    Filed: December 15, 2009
    Publication date: September 22, 2011
    Applicant: MERCK SERONO S.A.
    Inventors: Mathilde Muzerelle, Anna Quattropani, Cyril Montagne, Jérôme Dorbais
  • Publication number: 20110201581
    Abstract: The present invention provides compounds of formula (I) in which n, y, X1, X2, A, B, R1, R2, R3, R4 and R5 are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Application
    Filed: February 11, 2011
    Publication date: August 18, 2011
    Inventors: Mark Furber, Christopher Andrew Luckhurst, Hitesh Jayantilal Sanganee, Linda Anne Stein, Peter Alan Cage
  • Publication number: 20110160186
    Abstract: The invention provides various methods comprising the administration of a CYP2D6 bioactive drug covalently bound to a water-soluble oligomer. Metabolism of CYP2D6 bioactive drug conjugates is diverted from CYP2D6 to alternative pathways, and the conjugates may therefore be utilized to alleviate the problems associated with interpopulation variation resulting from the genetic polymorphism in the CYP2D6 gene.
    Type: Application
    Filed: June 9, 2009
    Publication date: June 30, 2011
    Applicant: Nektar Therapeutics
    Inventors: Michael A. Eldon, C. Simone Jude-Fishburn, Hema Gursahani, Myong Gyong Lee
  • Publication number: 20110124625
    Abstract: The present invention provides compounds having formula (I): and pharmaceutically acceptable derivatives thereof, wherein R1-R4, n, p, A, B, D, E, L and AR1 are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of disorders mediated by the CD11/CD18 family of cellular adhesion molecules (e.g., LFA-1).
    Type: Application
    Filed: February 4, 2011
    Publication date: May 26, 2011
    Applicant: SARcode Corporation
    Inventors: Wang Shen, Kenneth Barr, Johan D. Oslob, Min Zhong
  • Patent number: 7897618
    Abstract: Disclosed are N-aroyl cyclic amine derivatives having the formula: where the variables are as define herein, and their use as pharmaceuticals, specifically as orexin receptor antagonists.
    Type: Grant
    Filed: October 29, 2007
    Date of Patent: March 1, 2011
    Assignee: SmithKline Beecham Limited
    Inventors: Clive Leslie Branch, Wai Ngor Chan, Amanda Johns, Christopher Norbert Johnson, David John Nash, Riccardo Novelli, Jean-Pierre Pilleux, Roderick Alan Porter, Rachel Elizabeth Anne Stead, Geoffrey Stemp
  • Publication number: 20110009446
    Abstract: The invention relates to (among other things) oligomer-guanidine class conjugates and related compounds. A conjugate of the invention, when administered by any of a number of administration routes, exhibits advantages over previously administered compounds.
    Type: Application
    Filed: January 9, 2009
    Publication date: January 13, 2011
    Applicant: Nektar Therapeutics
    Inventors: Wen Zhang, Stephanie Allums, Jennifer Riggs-Sauthier
  • Publication number: 20100298374
    Abstract: Disclosed are nitrile derivatives and pharmaceutical compositions comprising nitrile derivatives. The pharmaceutical compositions comprise compounds of the formula I and the pharmaceutically acceptable salts of such compounds. Also disclosed are processes for the preparation of such compounds, intermediates used in the preparation of such compounds, and the uses of such compounds in treating hyperproliferative diseases, inflammatory diseases and viral and bacterial infections and inducing apoptosis in cancer cells.
    Type: Application
    Filed: May 14, 2010
    Publication date: November 25, 2010
    Applicant: CELLCEUTIX CORPORATION
    Inventor: Krishna MENON
  • Publication number: 20100273827
    Abstract: The present invention relates to novel oxadiazole derivatives having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.
    Type: Application
    Filed: December 19, 2008
    Publication date: October 28, 2010
    Inventor: Jag Paul Heer
  • Patent number: 7816352
    Abstract: The present invention provides compounds that act as selective agents to protect against unintentional cell death or tissue damage and can relieve side effects of cancer treatment such as, for example, oral mucositis, hair loss, diarrhea due to damage to the gastrointestinal epithelium, and myelosuppression. In addition, these compounds can be used to prevent premature cell death when the cell death is caused by signals from damaged cells, for example, signals generated as the result of a traumatic incident or an ischemic episode.
    Type: Grant
    Filed: March 10, 2006
    Date of Patent: October 19, 2010
    Assignee: The Regents of The University of California
    Inventors: Dennis A. Carson, Howard B. Cottam, Sylvie Barchéchath, Mary Patricia Corr
  • Patent number: 7767670
    Abstract: The invention provides methods and compositions for treating conditions mediated by various kinases wherein substituted 3-carboxamido isoxazoles compounds are employed. The invention also provides methods of using the compounds and/or compositions in the treatment of a variety of diseases and unwanted conditions in subjects.
    Type: Grant
    Filed: November 15, 2004
    Date of Patent: August 3, 2010
    Assignee: Ambit Biosciences Corporation
    Inventors: Shamal A. Mehta, Robert M. Grotzfeld, Zdravko V. Milanov, Andiliy G. Lai, Hitesh K. Patel, David J. Lockhart
  • Publication number: 20100190822
    Abstract: The present invention relates to compounds which inhibit dipeptidyl peptidase IV (DPP-IV) and are useful for the prevention or treatment of diabetes, especially type II diabetes, as well as hyperglycemia, Syndrome X, hyperinsulinemia, obesity, atherosclerosis, and various immunomodulatory diseases.
    Type: Application
    Filed: March 19, 2010
    Publication date: July 29, 2010
    Applicant: ABBOTT LABORATORIES
    Inventors: David J. Madar, Stevan W. Djuric, Melissa J. Michmerhuizen, Hana A. Kopecka, Xiaofeng Li, Kenton L. Longenecker, Zhonghua Pei, Daisy Pireh, Hing L. Sham, Kent D. Stewart, Bruce G. Szczepankiewicz, Paul E. Wiedeman, Hong Yong
  • Publication number: 20090170895
    Abstract: The present invention relates to a medicine, and more particularly to novel arylamidrazone derivatives having an antagonistic action against S1P3 receptors and a medicine containing thereof as an active ingredient.
    Type: Application
    Filed: October 11, 2006
    Publication date: July 2, 2009
    Applicant: TOA EIYO LTD.
    Inventors: Shin-ya Ohnuma, Takeshi Hasegawa, Tomoyuki Sada
  • Patent number: 7547783
    Abstract: A transition metal complex which is a bis-arylimine pyridine MXn complex or a [bis-arylimine pyridine MXp+][NC?]q complex comprising a bis-arylimine pyridine ligand and M is a transition metal atom; n matches the formal oxidation state of the transition metal atom M; X is halide, optionally substituted hydrocarbyl, alkoxide, amide, or hydride; NC? is a non-coordinating anion; and p+q matches the formal oxidation state of the transition metal atom M. The transition metal complexes of the present invention, their complexes with non-coordinating anions and catalyst systems containing such complexes have good solubility in non-polar media and chemically inert non-polar solvents especially aromatic hydrocarbon solvents. The catalyst systems can be used for a wide range of (co-)oligomerization, polymerization and dimerization reactions.
    Type: Grant
    Filed: March 23, 2005
    Date of Patent: June 16, 2009
    Assignee: Shell Oil Company
    Inventors: Eric Johannes Maria De Boer, Harry Van Der Heijden, Quoc An On, Johan Paul Smit, Arie Van Zon
  • Patent number: 7511059
    Abstract: The invention relates to thiazolidinones of general formula (I) their production and use as inhibitors of polo-like kinases (Plk) for treating various diseases.
    Type: Grant
    Filed: February 2, 2006
    Date of Patent: March 31, 2009
    Assignee: Schering Ag
    Inventors: Volker Schulze, Knut Eis, Lars Wortmann, Dirk Kosemund, Olaf Prien, Gerhard Siemeister, Holger Hess-Stumpp, Uwe Eberspaecher, Damian O Arnaiz
  • Patent number: 7429667
    Abstract: The invention concerns compounds which inhibit MEK and which have activity as anti-neoplastic agents. These compounds include N-substituted-3-hydroxy-5-arylamino-isothiazole-4-carboxamidines. Also included are the tautomeric isothiazol-3(2H)-ones.
    Type: Grant
    Filed: January 20, 2006
    Date of Patent: September 30, 2008
    Assignee: Ardea Biosciences, Inc.
    Inventors: Hassan Abdellaoui, Robert Tam, Huanming Chen, Varaprasad Chamakura, Dinesh Barawkar, Andreas Maderna, Zhi Hong, Stanley Lang
  • Patent number: 7157468
    Abstract: This invention relates to pyrazole derivatives of formula (I) or pharmaceutically acceptable salts, solvates or derivative thereof, wherein R1 to R4, n W, X and Y are defined in the description, and to processes for the preparation thereof, intermediates used in their preparation of, compositions containing them and the uses of such derivatives. The compounds of the present invention bind to the enzyme reverse transcriptase and are modulators, especially inhibitors thereof. As such the compounds of the present invention are useful in the treatment of a variety of disorders including those in which the inhibition of reverse transcriptase is implicated. Disorders of interest include those caused by Human Immunodificiency Virus (HIV) and genetically related retroviruses, such as Acquired Immune Deficiency Syndrome (AIDS).
    Type: Grant
    Filed: September 23, 2003
    Date of Patent: January 2, 2007
    Assignee: Pfizer Inc.
    Inventors: Lyn Howard Jones, Charles Eric Mowbray, David Anthony Price, Matthew Duncan Selby, Paul Anthony Stupple
  • Patent number: 7030150
    Abstract: The present invention relates to novel benzimidazole compounds that have useful antiviral activity. More specifically, the invention encompasses benzimidazole compounds that inhibit membrane fusion associated events such as viral transmission, reduce viral load or otherwise treat viral infections. The invention also encompasses the use of benzimidazole compounds as inhibitors of membrane fusion associated events, such as viral transmission. In another embodiment, the invention encompasses processes for making benzimidazole compounds, methods of using the benzimidazole compounds and compositions comprising the benzimidazole compounds. Finally, the invention provides methods for treating, preventing or ameliorating symptoms associated with respiratory infection, particularly that caused by Respiratory Syncytial Virus utilizing the novel benzimidazole compounds of the invention.
    Type: Grant
    Filed: May 9, 2002
    Date of Patent: April 18, 2006
    Assignee: Trimeris, Inc.
    Inventors: John William Lackey, Daniel S Kinder, Nicolai A Tvermoes
  • Patent number: 6855717
    Abstract: Compounds of formula (I): wherein: R2 represents a hydrogen atom or a C1-4alkyl group; q is 1 or 2; A represents a group of formula (a) or (b) wherein T, U, V and Y independently represent CH or a nitrogen atom; R5 is a group selected from: a hydrogen or halogen atom, cyano, C1-4 alkyl or C1-4 alkoxy group s is 1 or 2; Ar2 represents an optionally substituted phenyl ring or an optionally substituted 5- or 6-membered aromatic heterocyclic ring; and salts thereof. The compounds are useful for the treatment of conditions which require modulaton of a dopamine receptor such as schizophrenia.
    Type: Grant
    Filed: February 14, 2003
    Date of Patent: February 15, 2005
    Assignee: SmithKline Beecham, plc
    Inventors: Clive Leslie Branch, Christopher Norbert Johnson, Geoffrey Stemp
  • Patent number: 6849617
    Abstract: The invention includes pharmaceutically active compounds and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are particularly useful for treating or prophylaxis of undesired thrombosis.
    Type: Grant
    Filed: May 23, 2003
    Date of Patent: February 1, 2005
    Assignee: Sunol Molecular Corporation
    Inventors: Jin-An Jiao, Lawrence K. Luepschen, Esperanza L. Nieves, Hing C. Wong, Dean P. Taylor
  • Patent number: 6825213
    Abstract: The invention provides &bgr;3-adrenoreceptor agonists, pharmaceutical compositions comprising &bgr;3-adrenoreceptor agonist compounds, and methods of using such compounds for stimulating, regulating or modulating metabolism of fats in adipose tissue in animals.
    Type: Grant
    Filed: June 25, 2003
    Date of Patent: November 30, 2004
    Assignee: Molecular Design International, Inc.
    Inventors: Dennis R. Feller, Duane D. Miller
  • Patent number: 6770657
    Abstract: The invention relates to novel isoquinolines and their use as anticonvulsant and in the treatment of a variety of disorders.
    Type: Grant
    Filed: September 11, 2002
    Date of Patent: August 3, 2004
    Assignee: Smithkline Beecham p.l.c.
    Inventors: John David Harling, Mervyn Thompson
  • Patent number: 6730783
    Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.
    Type: Grant
    Filed: April 22, 2003
    Date of Patent: May 4, 2004
    Assignee: 3-Dimensional Pharmaceuticals, Inc.
    Inventors: Bruce E. Tomczuk, Richard M. Soll, Tianbao Lu, Cynthia L. Fedde, Carl R. Illig, Thomas P. Markotan
  • Publication number: 20040030131
    Abstract: A compound of the formula in which R1 and R2 are each hydrogen or C1-4 alkyl, or R1 and R2 together with the nitrogen atom to which they are attached form an azetidinyl, pyrrolidinyl, piperidinyl, piperazinyl or morpholino group, said group being optionally substituted with 1 to 3 substituents selected from C1-4 alkyl, hydroxymethyl, C1-4 alkoxymethyl and amido, R3 is a naphthyl, indolyl, benzothienyl, benzofuranyl, benzothiazolyl, quinolinyl or isoquinolinyl group, said group being optionally substituted, and n is 1 or 2; and m is 0 or 1, provided that when m is 1 then n is 1; or a salt or ester thereof.
    Type: Application
    Filed: September 3, 2003
    Publication date: February 12, 2004
    Inventors: Martine Keenan, Vincent Patrick Rocco, Kumiko Takeuchi, David Edward Tupper, Vincent Vivien
  • Publication number: 20040019079
    Abstract: The invention provides &bgr;3-adrenoreceptor agonists, pharmaceutical compositions comprising &bgr;3-adrenoreceptor agonist compounds, and methods of using such compounds for stimulating, regulating or modulating metabolism of fats in adipose tissue in animals.
    Type: Application
    Filed: June 25, 2003
    Publication date: January 29, 2004
    Inventors: Dennis R. Feller, Duane D. Miller
  • Patent number: 6638931
    Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.
    Type: Grant
    Filed: November 28, 2000
    Date of Patent: October 28, 2003
    Assignee: 3-Dimensional Pharmaceuticals, Inc.
    Inventors: Bruce E. Tomczuk, Richard M. Soll, Tianbao Lu, Cynthia L. Fedde, Carl R. Illig, Thomas P. Markotan, Thomas P. Stagnaro
  • Patent number: 6602864
    Abstract: The compounds of formula I herein exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More specifically, they are inhibitors of the activity of Factor Xa. The present invention is directed to compounds of formula I, compositions containing compounds of formula I, and their use, which are for treating a patient suffering from, or subject to, physiological condition which can be ameliorated by the administration of an inhibitor of the activity of Factor Xa.
    Type: Grant
    Filed: June 3, 1998
    Date of Patent: August 5, 2003
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Yong Mi Choi-Sledeski, Henry W. Pauls, Jeffrey N. Barton, William R. Ewing, Daniel M. Green, Michael R. Becker, Yong Gong
  • Patent number: 6602867
    Abstract: Triazole compounds of the following formula where R1, R2, A and B have the meanings given in the description are described. The compounds according to the invention possess a high affinity for the dopamine D3 receptor and can therefore be used for treating diseases which respond to the influence of dopamine D3 ligands.
    Type: Grant
    Filed: July 11, 2001
    Date of Patent: August 5, 2003
    Assignee: Abbott Laboratories
    Inventors: Dorothea Starck, Hans-Jörg Treiber, Liliane Unger, Barbara Neumann-Schultz, Kai Blumbach, Dietmar Schöbel
  • Patent number: 6596752
    Abstract: The present invention relates to small molecules according to the formula [I]: which are potent inhibitors of &agr;4&bgr;1 mediated adhesion to either VCAM or CS-1 and which can be used for treating or preventing &agr;4&bgr;1 adhesion mediated conditions in a mammal such as a human.
    Type: Grant
    Filed: July 12, 2002
    Date of Patent: July 22, 2003
    Assignees: Tanabe Seiyaku Co., Ltd., Pharmacia & Upjohn Company
    Inventors: Thomas J. Lobl, Bradley R. Teegarden, Alexander Polinsky, Gilbert M. Rishton, Masafumi Yamagishi, Steven Tanis, Jed F. Fisher, Edward W. Thomas, Robert A. Chrusciel
  • Patent number: 6562828
    Abstract: A compound of the formula [I] wherein R1, R2 and R3 are the same or different and each is hydrogen atom, wherein each symbol is as defined in the specification, a salt thereof or a prodrug thereof. The compound of the present invention, a salt thereof and a prodrug thereof are useful as factor Xa inhibitor and blood coagulation inhibitor, and are useful for the prophylaxis and/or treatment of diseases caused by blood coagulation or thrombus.
    Type: Grant
    Filed: October 6, 2000
    Date of Patent: May 13, 2003
    Assignee: Japan Tobacco Inc.
    Inventors: Susumu Katoh, Katsuyuki Yokota, Mikio Hayashi
  • Patent number: 6541632
    Abstract: A carbocyclic or heterocyclic compound, ammonia and an oxygen-containing gas are subjected to fluid catalytic reaction in vapor phase in the presence of a catalyst containing alkali metal to produce an aromatic or heterocyclic nitrile. The use of the catalyst containing a specific amount of alkali metal enables the stable production of the aromatic or heterocyclic nitrile in high yields with little change with time even when water is present in the reaction system. The use of the catalyst containing the alkali metal also enables the recycle and reuse of unreacted ammonia which is usually accompanied by water, thereby reducing production costs.
    Type: Grant
    Filed: June 19, 2002
    Date of Patent: April 1, 2003
    Assignee: Mitsubishi Gas Chemical Company, Inc.
    Inventors: Hideaki Ogino, Takashi Okawa, Shuji Ebata, Yoshinori Kanamori
  • Patent number: 6518310
    Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.
    Type: Grant
    Filed: March 16, 2001
    Date of Patent: February 11, 2003
    Assignee: 3-Dimensional Pharmaceuticals, Inc.
    Inventors: Bruce E. Tomczuk, Richard M. Soll, Tianbao Lu, Cynthia L Fedde, Carl R Illig, Thomas P. Markotan, Thomas P Stagnaro