Additional Nitrogen Containing Hetero Ring (e.g., Thiazetidine, Etc.) Patents (Class 544/111)
  • Publication number: 20120101080
    Abstract: The invention relates to a pharmaceutical composition comprising a compound of formula (1) wherein R1 is optionally substituted phenyl, optionally substituted pyridyl or optionally substituted indolyl; R2 is (CH2)n wherein n is 0, 1, 2, 3 or 4; R3 is (CH2)mR3A wherein m is 0, 1, 2, 3 or 4, and R3A is methyl, isopropyl, tert-butyl, OCH3, OH, optionally substituted phenoxy, C?CH, C?N, optionally substituted phenyl, furanyl or thienyl; A is a ring containing X1 with the meaning O, S, NH, N(CH3) or CH2; and X2 is O, S or NH; and a compound of formula (2) wherein R4 is optionally substituted phenyl, optionally substituted pyridyl, optionally substituted indolyl, —NR7R8; or —NH—N?CH—R9; and substituents R5 to R9 have the meanings indicated in the description, in particular ethionamide. The pharmaceutical composition is useful, e.g., in the treatment of multidrug-resistant tuberculosis.
    Type: Application
    Filed: June 25, 2010
    Publication date: April 26, 2012
    Applicant: BioVersys AG
    Inventors: Ronald Schoenmakers, Wilfried Weber, Marc Gitzinger, Martin Fussenegger, Marcel Tigges, Peter Schneider
  • Patent number: 8158622
    Abstract: Compounds represented by Formula (I): or pharmaceutically acceptable salts thereof, are inhibitors of glycogen phosphorylase and are useful in the prophylactic or therapeutic treatment of diabetes, hyperglycemia, hypercholesterolemia, hyperinsulinemia, hyperlipidemia, hypertension, atherosclerosis or tissue ischemia e.g. myocardial ischemia, and as cardioprotectants.
    Type: Grant
    Filed: July 2, 2008
    Date of Patent: April 17, 2012
    Assignee: Prosidion Limited
    Inventors: Stuart Edward Bradley, Thomas Martin Krulle, Peter John Murray, Martin James Procter, Robert John Rowley, Colin Peter Sambrook Smith, Gerard Hugh Thomas, Karen Lesley Schofield
  • Patent number: 8153631
    Abstract: The present invention provides a triazole compound of the following formula: a prodrug thereof or a pharmaceutically acceptable salt thereof. The above-mentioned triazole compound has superior HSD1 inhibitory activity, and is useful as an HSD1 inhibitor, a therapeutic drug of diabetes or a therapeutic drug of obesity or a therapeutic drug of metabolic syndrome.
    Type: Grant
    Filed: November 19, 2009
    Date of Patent: April 10, 2012
    Assignee: Amgen Inc.
    Inventors: Jay P. Powers, Mario G. Cardozo, Hiroyuki Goto, Kazuhito Harada, Katsuaki Imamura, Makoto Kakutani, Isamu Matsuda, Yasuhiro Ohe, Shinji Yata
  • Patent number: 8143393
    Abstract: This invention relates to novel pyrrozolotriazine compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.
    Type: Grant
    Filed: December 1, 2006
    Date of Patent: March 27, 2012
    Assignee: Bayer HealthCare LLC
    Inventors: Julie A. Dixon, Barton Phillips, Furahi Achebe, Harold C. E. Kluender, Jason Newcom, Kyle Parcella, Steven Magnuson, Zhenqiu Hong, Zhonghua Zhang, Zheng Liu, Uday Khire, Lei Wang, Martin Michels, Brent Chandler, Stephen O'Connor
  • Patent number: 8129379
    Abstract: This invention relates to novel pyrrozolotriazine compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.
    Type: Grant
    Filed: September 2, 2009
    Date of Patent: March 6, 2012
    Assignee: Bayer HealthCare LLC
    Inventors: Julie A. Dixon, Barton Phillips, Furahi Achebe, Harold C. E. Kluender, Jason Newcom, Kyle Parcella, Steven Magnuson, Zhenqiu Hong, Zhonghua Zhang, Zheng Liu, Uday Khire, Lei Wang, Martin Michels, Brent Chandler, Stephen O'Connor
  • Publication number: 20120010189
    Abstract: Disclosed herein are azetidinyl compounds of formula I, as described herein, pharmaceutical compositions comprising an azetidinyl compound, and a method of using an azetidinyl compound in the treatment or prophylaxis of a melanin-concentrating hormone related disease or condition.
    Type: Application
    Filed: July 5, 2011
    Publication date: January 12, 2012
    Applicant: AstraZeneca AB
    Inventors: Susanne Doris Margit Bökman-Winiwarter, Marlene FREDENWALL, Carl Anders Hogner, Lars Anders Mikael Johansson, Robert Andrew Judkins, Lanna Li, Björn Christian Ingvar Löfberg, Sverker Von Unge
  • Patent number: 8093389
    Abstract: The invention relates to a compound of a general formula (I): wherein Ar1 represents a group formed from an aromatic ring selected from a group consisting of indole, 1H-indazole, 2H-indazole, 1H-thieno[2,3-c]pyrazole, 1H-pyrazolo[3,4-b]pyridine, benzo[b]furan, benzimidazole, benzoxazole, 1,2-benzisoxazole and imidazo[1,2-a]pyridine; R1 and R2 each represent a hydrogen atom, a halogen atom, a cyano group, a C2-C6 alkenyl group, a C1-C6 alkoxy group, a halo-C1-C6 alkoxy group, a cyclo-C3-C6 alkyloxy group, a C2-C7 alkanoyl group, a halo-C2-C7 alkanoyl group, a C2-C7 alkoxycarbonyl group, a halo-C2-C7 alkoxycarbonyl group, a cyclo-C3-C6 alkyloxycarbonyl group, an aralkyloxycarbonyl group, a carbamoyl-C1-C6 alkoxy group, a carboxy-C2-C6 alkenyl group, or a group of -Q1-N(Ra)-Q2-Rb; an optionally-substituted C1-C6 alkyl, aryl or heterocyclic group; or a C1-C6 alkyl or C2-C6 alkenyl group having the aryl or heterocyclic group; R3 and R4 each represent a hydrogen atom, a halogen atom, a nitro group, a cyclo-C3-C
    Type: Grant
    Filed: January 8, 2008
    Date of Patent: January 10, 2012
    Assignees: Merck Sharp & Dohme Corp., MSD K.K.
    Inventors: Tomoharu Iino, Hideki Jona, Jun Shibata, Tadashi Shimamura, Takeru Yamakawa, Lihu Yang
  • Patent number: 8088925
    Abstract: The present invention relates to compounds of the formula I, which exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses.
    Type: Grant
    Filed: November 15, 2007
    Date of Patent: January 3, 2012
    Assignee: Sanofi-Aventis
    Inventors: Michael Wagner, Matthias Urmann, Volkmar Wehner, Martin Lorenz, Armin Bauer, Marc Nazare, Hans Matter
  • Patent number: 8084618
    Abstract: Heterocyclic compounds derived from benzotriazine, triazines, triazoles and oxadiazoles are disclosed. The methods of synthesis and of use of such heterocyclic compounds are also provided.
    Type: Grant
    Filed: January 8, 2010
    Date of Patent: December 27, 2011
    Assignee: TargeGen, Inc.
    Inventors: Wolfgang Wrasidlo, Elena Dneprovskaia
  • Patent number: 8076330
    Abstract: The present invention relates generally to pyrrolidine and thiazolidine DPP-IV inhibitor compounds. The present invention also provides synthetic methods for preparation of such compounds, methods of inhibiting DPP-IV using such compounds and pharmaceutical formulations containing them for treatment of DPP-IV mediated diseases, in particular, Type-2 diabetes.
    Type: Grant
    Filed: January 13, 2011
    Date of Patent: December 13, 2011
    Assignee: Amgen Inc.
    Inventors: Heiko Kroth, Tim Feuerstein, Frank Richter, Jürgen Boer, Michael Essers, Bert Nolte, Matthias Schneider, Matthias Hochgürtel, Fritz-Frieder Frickel, Arthur G. Taveras, Christoph Steeneck
  • Publication number: 20110263558
    Abstract: Disclosed are compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof. Such compounds are MEK inhibitors and are useful in the treatment of proliferative diseases, such as cancer. Also disclosed are pharmaceutical compositions containing such compounds as well as methods of using the compounds and compositions of the invention in the treatment of cancer.
    Type: Application
    Filed: March 15, 2011
    Publication date: October 27, 2011
    Applicant: EXELIXIS, INC.
    Inventors: Naing Aay, Neel Kumar Anand, Charles M. Blazey, Owen Joseph Bowles, Joerg Bussenius, Simona Costanzo, Jeffry Kimo Curtis, Steven Charles DeFina, Larisa Dubenko, Anagha Abhijit Joshi, Abigail R. Kennedy, Angie Inyoung Kim, Elena S. Koltun, Jean-Claire Limun Manalo, Csaba J. Peto, Kenneth D. Rice, Tsze H. Tsang
  • Patent number: 8039467
    Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, TNF-? or combinations thereof.
    Type: Grant
    Filed: October 20, 2009
    Date of Patent: October 18, 2011
    Assignee: Schering Corporation
    Inventor: Chaoyang Dai
  • Patent number: 8017604
    Abstract: The invention is concerned with novel imidazopyridine derivatives of formula (I) wherein R1, R2, R3, R4, R5 and A are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used for the treatment of various diseases, including central nervous system disorders such as Alzheimer's disease, Parkinson's disease, and schizophrenia.
    Type: Grant
    Filed: September 21, 2010
    Date of Patent: September 13, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Daniela Alberati, Rubén Alvarez Sánchez, Konrad Bleicher, Alexander Flohr, Katrin Groebke Zbinden, Matthias Koerner, Bernd Kuhn, Jens-Uwe Peters, Markus Rudolph
  • Patent number: 8017769
    Abstract: Benzazole substituted aminobenzenesulfonate derivatives of formula (A) (wherein X, Q and M are as defined in the specification) are useful as components of water-soluble fluorescent inks and dyes invisible in day-light. Novel intermediates for the above compounds are also disclosed.
    Type: Grant
    Filed: July 26, 2006
    Date of Patent: September 13, 2011
    Inventors: Boris Markovich Bolotin, Yevgeniy Alexeyevich Birgen, Maria Leonardovna Kukushkina, Yelena Viktorovna Yakovleva
  • Publication number: 20110212940
    Abstract: The present invention relates to compounds of the general formula (I) that have activity as S1P receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate S1P receptor activity. The compounds may be used as immunomodulators, e.g., for treating or preventing diseases such as autoimmune and related immune disorders including systemic lupus erythematosus, inflammatory bowel diseases such as Crohn's disease and ulcerative colitis, type I diabetes, uveitis, psoriasis, myasthenia gravis, rheumatoid arthritis, non-glomerular nephrosis, hepatitis, Behçet's disease, glomerulonephritis, chronic thrombocytopenic purpura, hemolytic anemia, hepatitis and Wegner's granuloma; and for treating other conditions.
    Type: Application
    Filed: February 25, 2011
    Publication date: September 1, 2011
    Applicant: EPIX PHARMACEUTICALS, INC.
    Inventors: Roland Burli, Victor J. Cee, Jennifer Golden, Brian Alan Lanman, Susana Neira, Ashis Saha, Nili Schutz, Xiang Yu, Dilara McCauley, Mercedes Lobera, Yael Marantz, Jian Lin, Srinivasa R. Cheruku, Pini Orbach, Anurag Sharadendu, Robert C. Penland, Kimberley Gannon, Sharon Shacham, Silvia Noiman, Oren Becker, Zhaoda Zhang
  • Patent number: 8003643
    Abstract: The present invention is directed to compounds which contain substituted pyridazines and pyrimidines moieties which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.
    Type: Grant
    Filed: November 18, 2009
    Date of Patent: August 23, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Mark T. Bilodeau, Peter C. Chua, Nicholas D. P. Cosford, Jacob M. Hoffman, Johnny Yasuo Nagasawa
  • Patent number: 7982036
    Abstract: The present invention provides compounds of formula I wherein Ring A, Ring B, m, Rx, Ry, W and R1 are as defined herein, pharmaceutically acceptable salts and compositions thereof, and methods of using the same.
    Type: Grant
    Filed: October 17, 2008
    Date of Patent: July 19, 2011
    Assignee: Avila Therapeutics, Inc.
    Inventors: Juswinder Singh, Shomir Ghosh, Arthur F. Kluge, Russell C. Petter, Richland W. Tester
  • Patent number: 7976739
    Abstract: A chromene compound represented by the following formula (1), wherein, “A” is an annulated ring, R1 and R2 are hydrogen atoms, hydroxyl groups or the like groups, R3, R4, R5 and R6 are substituents such as hydroxyl groups or the like groups, “a” and “b” are, respectively, integers of 0 to 4, and “c” and “d” are, respectively, integers of 0 to 5. The chromene compound is a photochromic compound developing a color of a neutral tint, and has a high color density per a unit amount.
    Type: Grant
    Filed: August 22, 2007
    Date of Patent: July 12, 2011
    Assignee: Tokuyama Corporation
    Inventors: Shinobu Izumi, Junji Takenaka
  • Publication number: 20110129678
    Abstract: Described herein are compounds generally comprising an indeno[2?,3?:3,4]naptho[1,2-b]pyran structure. Such compounds may be useful for their photochromic properties, and be used in certain photochromic compositions. Such compositions may further comprise other photochromic compositions and/or materials. Additionally, such compounds and/or compositions may be suitable for preparing certain photochromic articles. Also described herein are methods for preparing certain photochromic compounds, compositions, and articles.
    Type: Application
    Filed: December 16, 2010
    Publication date: June 2, 2011
    Applicant: Transitions Optical, Inc.
    Inventors: Meng He, Darrin R. Dabideen, Anil Kumar, Ruisong Xu
  • Patent number: 7943649
    Abstract: The invention encompasses novel compounds of Formula I or pharmaceutically acceptable salts thereof. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful to treat pain and/or inflammation from a variety of diseases or conditions, such as osteoarthritis, rheumatoid arthritis and acute or chronic pain. Methods of treating diseases or conditions mediated by the mPGES-1 enzyme and pharmaceutical compositions are also encompassed.
    Type: Grant
    Filed: October 24, 2008
    Date of Patent: May 17, 2011
    Assignee: Merck Frosst Canada Ltd.
    Inventors: Anh Chau, Bernard Cote, Yves Ducharme, Richard Frenette, Richard Friesen, Marc Gagnon, Andre Giroux, Evelyn Martins, Hongping Yu, Tom Wu
  • Patent number: 7935725
    Abstract: Aryl-substituted bridged or fused diamine compounds, pharmaceutical compositions containing them, and methods of using the compounds and the pharmaceutical compositions for leukotriene A4 hydrolase (LTA4H or LTA4H) modulation and for the treatment of disease states, disorders, and conditions mediated by LTA4H activity, such as allergy, asthma, autoimmune diseases, pruritis, inflammatory bowel disease, ulcerative colitis, and cardiovascular disease, including atherosclerosis and prevention of myocardial infarction.
    Type: Grant
    Filed: October 30, 2008
    Date of Patent: May 3, 2011
    Assignee: Janssen Pharmaceutica NV
    Inventors: Scott D. Bembenek, Wendy Eccles, Laurent Gomez, Cheryl A. Grice, Aaron M. Kearney, Adrienne M. Landry-Bayle, Taraneh Mirzadegan, Alejandro Santillán, Jr.
  • Patent number: 7935696
    Abstract: A compound of Formula I and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof. Also disclosed are pharmaceutical compositions containing compounds of Formula I, and methods of treating conditions associated with the activity of p38 kinase.
    Type: Grant
    Filed: October 25, 2007
    Date of Patent: May 3, 2011
    Assignee: Bristol-Myers Squibb Company
    Inventors: Stephen T. Wrobleski, Jagabandhu Das, T. G. Murali Dhar, Alaric J. Dyckman, John Hynes, Katerina Leftheris, James Lin, Shuqun Lin
  • Patent number: 7928103
    Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
    Type: Grant
    Filed: October 15, 2007
    Date of Patent: April 19, 2011
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Doris Riether, David Smith Thomson, Renee M. Zindell
  • Patent number: 7919528
    Abstract: Novel PDF inhibitors and novel methods for their use are provided.
    Type: Grant
    Filed: May 30, 2003
    Date of Patent: April 5, 2011
    Assignee: GlaxoSmithKline LLC
    Inventors: Kelly M. Aubart, Andrew B. Benowitz, Siegfried B. Christensen, IV, Joseph M. Karpinski, Jinhwa Lee, Domingos J. Silva
  • Patent number: 7893257
    Abstract: The present invention is directed to a novel process for the preparation of piperazinyl and diazepanyl benzamide derivatives, useful for the treatment of disorders and conditions mediated by a histamine receptor, preferably the H3 receptor.
    Type: Grant
    Filed: December 10, 2007
    Date of Patent: February 22, 2011
    Assignee: Janssen Pharmaceutica NV
    Inventors: Anusuya Choudhury, Jeffrey S. Grimm, Kirk L. Sorgi, David Palmer, Jing Liu
  • Patent number: 7893062
    Abstract: The invention relates to pyrrolidine derivatives of formula wherein R1, R2, R3, n, and o are defined in the specification and to pharmaceutically active acid-addition salts thereof. Compounds of formula I have a high affinity simultaneously to both the NK1 and the NK3 receptors (dual NK1/NK3 receptor antagonists), useful in the treatment of schizophrenia.
    Type: Grant
    Filed: April 14, 2008
    Date of Patent: February 22, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Caterina Bissantz, Torsten Hoffmann, Philippe Jablonski, Henner Knust, Matthias Nettekoven, Hasane Ratni, Xihan Wu
  • Patent number: 7888379
    Abstract: The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.
    Type: Grant
    Filed: May 24, 2006
    Date of Patent: February 15, 2011
    Assignee: Merck Serono SA
    Inventors: Anna Quattropani, David Covini, Vincent Pomel, Jerome Dorbais, Thomas Rueckle
  • Patent number: 7884101
    Abstract: The present invention relates to certain 3-phenyl-pyrazole derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor and are useful, optionally in combination with other pharmaceutical agents administered separately or together, in the treatment of platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, reducing the risk of blood clot formation, asthma or symptoms thereof, agitation or a symptom, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like.
    Type: Grant
    Filed: November 20, 2006
    Date of Patent: February 8, 2011
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Bradley Teegarden, Yifeng Xiong, Sonja Strah-Pleynet, Honnappa Jayakumar, Peter I. Dosa, Konrad Feichtinger, Martin Casper, Juerg Lehmann, Robert M. Jones, David J. Unett, Jin Sun Karoline Choi
  • Patent number: 7879888
    Abstract: The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.
    Type: Grant
    Filed: May 24, 2006
    Date of Patent: February 1, 2011
    Assignee: Merck Serono SA
    Inventors: Anna Quattropani, David Covini, Vincent Pomel, Jerome Dorbais, Thomas Rueckle
  • Patent number: 7875644
    Abstract: Compounds of the formula (I), in which R1, R2, R3a, R3b, R3c and R3d have the meanings indicated in claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumours.
    Type: Grant
    Filed: July 18, 2006
    Date of Patent: January 25, 2011
    Assignee: Merck Patent GmbH
    Inventors: Dieter Dorsch, Oliver Schadt, Andree Blaukat
  • Publication number: 20110009377
    Abstract: The invention relates to azetidine derivatives having the formula (I): Wherein R?, R1, R2, R3, R6, R7, R, Y, A and B are as defined herein. The invention also relates to a method for preparing the same and therapeutic use thereof.
    Type: Application
    Filed: June 18, 2010
    Publication date: January 13, 2011
    Applicant: SANOFI-AVENTIS
    Inventor: Jean-Francois Sabuco
  • Patent number: 7842808
    Abstract: The present invention relates to compounds of Formula (I) as antagonists of calcitonin gene-related peptide receptors (“CGRP-receptor”), pharmaceutical compositions comprising them, methods for identifying them, methods of treatment using them and their use in therapy for treatment of neurogenic vasodilation, neurogenic inflammation, migraine and other headaches, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors.
    Type: Grant
    Filed: January 5, 2007
    Date of Patent: November 30, 2010
    Assignee: Bristol-Myers Squibb Company
    Inventors: Prasad V. Chaturvedula, Ling Chen, Rita Civiello, Andrew P. Degnan, Gene M. Dubowchik, Xiaojun Han, Xiang Jun J. Jiang, Guanglin Luo, John E. Macor, Graham S. Poindexter, George O. Tora
  • Publication number: 20100249096
    Abstract: Disclosed are compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof. Such compounds are MEK inhibitors and are useful in the treatment of proliferative diseases, such as cancer. Also disclosed are pharmaceutical compositions containing such compounds as well as methods of using the compounds and compositions of the invention in the treatment of cancer.
    Type: Application
    Filed: May 5, 2010
    Publication date: September 30, 2010
    Applicant: EXELIXIS, INC.
    Inventors: Naing Aay, Neel Kumar Anand, Charles M. Blazey, Owen Joseph Bowles, Joerg Bussenius, Simona Costanzo, Jeffry Kimo Curtis, Steven Charles DeFina, Larisa Dubenko, Anagha Abhijit Joshi, Abigail R. Kennedy, Angie Inyoung Kim, Elena S. Koltun, Jean-Claire Limun Manalo, Csaba J. Peto, Kenneth D. Rice, Tsze H. Tsang
  • Patent number: 7803797
    Abstract: Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof, are disclosed, wherein G, B, Y, and A are as described. Methods, compositions, and medicaments related thereto are also disclosed.
    Type: Grant
    Filed: April 22, 2009
    Date of Patent: September 28, 2010
    Assignee: Allergan, Inc.
    Inventors: David W. Old, Vinh X. Ngo
  • Patent number: 7790721
    Abstract: Compounds of formula I where X is a bond; A1 and A2, together with the atoms to which they are attached, is pyrrole; and A3 and A4, together with the atoms to which they are attached, are benzene; are poly(ADP-ribose)polymerase inhibitors. The compounds of formula I are useful for the treatment of diseases such as cancer.
    Type: Grant
    Filed: December 27, 2007
    Date of Patent: September 7, 2010
    Assignee: Abbott Laboratories
    Inventors: Vincent L. Giranda, Julie M Miyashiro, Thomas D Penning, Keith W. Woods
  • Patent number: 7767673
    Abstract: Compounds represented by Formula (I): or a pharmaceutically acceptable salt or N-Oxide thereof, are useful in the treatment of cancer.
    Type: Grant
    Filed: September 12, 2008
    Date of Patent: August 3, 2010
    Assignee: OSI Pharmaceuticals, Inc.
    Inventors: Arlindo L. Castelhano, Andrew P. Crew, Han-Qing Dong, Radoslaw Laufer, An-Hu Li, Li Qiu, Colin Peter Sambrook Smith, Tao Zhang
  • Patent number: 7763629
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinase, represented by Structural Formula (I): wherein the variables in Structural Formula (I) are as described herein. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
    Type: Grant
    Filed: April 12, 2007
    Date of Patent: July 27, 2010
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jean-Damien Charrier, David Kay, Ronald Knegtel
  • Patent number: 7741343
    Abstract: Compounds of the formula I in which R1, R2, R3 and R4 are as defined in Claim 1, are ligands of the nicotinic acetylcholine receptor and/or serotonergic ligands and are suitable for the prophylaxis or treatment of psychoses, schizophrenia, depression, anxiety states, dementia, in particular Alzheimer's disease and Lewy bodies dementia, neurodegenerative disorders, Parkinson's disease, amyotrophic lateral sclerosis, Huntington's disease, Tourette's syndrome, learning and memory restrictions, bulimia, anorexia nervosa or other eating disorders, compulsive behavior, premenstrual syndrome, age-induced memory impairment, amelioration of withdrawal symptoms in nicotine dependence, strokes or brain damage by toxic compounds, and for the treatment of disorders which are characterized by an excess of circulating serotonin or by serotonergic hyperactivity.
    Type: Grant
    Filed: October 30, 2007
    Date of Patent: June 22, 2010
    Assignee: Merck Patent GmbH
    Inventors: Kai Schiemann, Henning Böttcher, Joachim Leibrock
  • Patent number: 7741316
    Abstract: A method of treating or preventing Alzheimer's disease, Parkinson's Disease and/or schizophrenia, this method comprising administering to a patient in need of such treatment a compound of formula: in which R, R3 and R4 are as defined in the specification.
    Type: Grant
    Filed: November 12, 2004
    Date of Patent: June 22, 2010
    Assignee: Aventis Pharma S.A.
    Inventors: Daniel Achard, Herve Bouchard, Jean Bouquerel, Bruno Filoche, Serge Grisoni, Augustin Hittinger, Michael R. Myers
  • Patent number: 7737141
    Abstract: The present invention provides a most suitable prodrug of a cinnamide compound. The prodrug is represented by Formula (I) wherein Ra and Rb each denote a C1-6 alkyl group or the like; Xa denotes a methoxy group or a fluorine atom; Y denotes a phosphono group or the like; and A denotes a cyclic lactam derivative.
    Type: Grant
    Filed: July 25, 2007
    Date of Patent: June 15, 2010
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Teiji Kimura, Koki Kawano, Noritaka Kitazawa, Nobuaki Sato, Toshihiko Kaneko, Koichi Ito, Mamoru Takaishi, Ikuo Kushida
  • Publication number: 20100137469
    Abstract: A photoactive compound that is the Michael addition reaction product of an aziridine compound and a photoinitiator-functional (meth)acrylate is described. The compound can be used to crosslink (meth)acrylic polymers via a hydrogen abstracting or an alpha-cleavage mechanism.
    Type: Application
    Filed: December 2, 2008
    Publication date: June 3, 2010
    Inventors: Peiwang Zhu, Maureen A. Kavanagh, Kelly S. Anderson, Larry R. Krepski, Guy D. Joly, Belma Erdogan, Babu N. Gaddam
  • Patent number: 7718798
    Abstract: The purpose of the present invention is to provide a glucokinase activator useful as a pharmaceutical agent such as an agent for the prophylaxis or treatment of diabetes, obesity and the like. The present invention provides a glucokinase activator containing a compound represented by the formula (I): wherein R1 is a hydrogen atom or a halogen atom; R2 is a group represented by wherein each symbol is defined in the specification, or a salt thereof or a prodrug thereof.
    Type: Grant
    Filed: March 19, 2009
    Date of Patent: May 18, 2010
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Tsuneo Yasuma, Osamu Ujikawa
  • Patent number: 7718679
    Abstract: The invention is concerned with novel heteroaryl carboxamides of formula (I) wherein A, R1, R2, X, Y, Z and m are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit the coagulation factor Xa and can be used for the treatment or prevention of thrombotic disorders.
    Type: Grant
    Filed: October 19, 2007
    Date of Patent: May 18, 2010
    Assignee: Hoffman-La Roche Inc.
    Inventors: Katrin Groebke Zbinden, Wolfgang Haap, Hans Hilpert, Bernd Kuhn, Narendra Panday, Fabienne Ricklin
  • Patent number: 7714150
    Abstract: Compounds corresponding to formula I, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and n have the meanings given in the description, and also a process for the preparation of these compounds and intermediate products of this process. Furthermore, pharmaceutical compositions comprising the compounds of Formula I and related methods of treatment.
    Type: Grant
    Filed: April 10, 2006
    Date of Patent: May 11, 2010
    Assignee: Solvay Pharmaceuticals GmbH
    Inventors: Brian Moloney, Lester Marrison, Dieter Ziegler, Michael Mlinaric, Christiane Boecker, Reinhard Brueckner, Michael Weske, Klaus Witte, Yvan Fischer
  • Patent number: 7700607
    Abstract: The present invention comprises a new class of compounds capable of modulating the c-kit receptor and, accordingly, useful for treatment of c-kit mediated diseases, including various inflammatory, fibrotic and/or mast cell mediated diseases such as mastocytosis. The compounds have a general Formula I wherein R1-6 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of c-kit mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.
    Type: Grant
    Filed: July 18, 2007
    Date of Patent: April 20, 2010
    Inventors: Essa Hu, Jason Brooks Human, Roxanne Kunz, Andrew Tasker, Ryan White
  • Publication number: 20100093694
    Abstract: The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.
    Type: Application
    Filed: September 4, 2009
    Publication date: April 15, 2010
    Inventors: Kap-Sun Yeung, Kyle E. Parcella, John A. Bender, Brett R. Beno, Katharine A. Grant-Young, Ying Han, Piyasena Hewawasam, John F. Kadow, Andrew Nickel
  • Patent number: 7696199
    Abstract: The invention relates to compounds of formula (I) having pharmacological activity towards the sigma receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which the sigma receptor is involved.
    Type: Grant
    Filed: August 29, 2005
    Date of Patent: April 13, 2010
    Assignee: Laboratorios del Dr. Esteve, S.A.
    Inventors: Christian Laggner, María Rosa Cuberes-Altisent, Joerg Holenz, Juana María Berrocal-Romero, María Montserrat Contijoch-Llobet
  • Patent number: 7683059
    Abstract: The present invention provides a triazole compound of the following formula: a prodrug thereof or a pharmaceutically acceptable salt thereof. The above-mentioned triazole compound is useful as a therapeutic drug for the treatment of diabetes, obesity or metabolic syndrome.
    Type: Grant
    Filed: September 5, 2006
    Date of Patent: March 23, 2010
    Assignee: Amgen Inc.
    Inventors: Mario G. Cardozo, Jay P. Powers, Hiroyuki Goto, Kazuhito Harada, Katsuaki Imamura, Makoto Kakutani, Isamu Matsuda, Yasuhiro Ohe, Shinji Yata
  • Publication number: 20100069346
    Abstract: The application relates to new piperazine- or morpholine-substituted azetidine derivatives of formula I. These compounds are antagonists at the neurokinin receptor and can be used for the treatment of gastrointestinal diseases. The application also relates to processes for the preparation of the compounds and to intermediates in said preparation.
    Type: Application
    Filed: June 21, 2006
    Publication date: March 18, 2010
    Inventors: Sara Holmqvist, Anders Chansson, Ame Svensson, Sverker Von Unge
  • Patent number: 7666863
    Abstract: The present invention relates to benzofuran derivatives and analogs, as well as compositions containing the same and to the use thereof for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by the hepatitis C virus.
    Type: Grant
    Filed: May 24, 2007
    Date of Patent: February 23, 2010
    Assignees: ViroPharma Incorporated, WYETH
    Inventors: Ashis K. Saha, Christopher J Burns, Alfred M. Del Vecchio, Thomas R. Bailey, Jason A. Reinhardt, Bheemashankar A. Kulkarni, Thomas H. Faitg, Hao Feng, Susan R. Rippin, Charles W. Blackledge, David J. Rys, Thomas A. Lessen, John Swestock, Yijun Deng, Theodore J. Nitz