The Five-membered Hetero Ring Consists Of Chalcogen, Plural Nitrogens, And Carbon Patents (Class 548/125)
  • Publication number: 20110152084
    Abstract: There are described N-(1,2,5-oxadiazol-3-yl)benzamides of the general formula (I) as herbicides. In this formula (I), X, Y, Z and R are radicals such as hydrogen, organic radicals such as alkyl, and other radicals such as halogen.
    Type: Application
    Filed: September 23, 2010
    Publication date: June 23, 2011
    Applicant: BAYER CROPSCIENCE AG
    Inventors: Arnim Köhn, Jörg Tiebes, Andreas Almsick, Hartmut Ahrens, Ines Heinemann, Rralf Braun, Monika H. Schmitt, Lothar Willms, Dieter Feucht, Christopher Hugh Rosinger, Isolde Häuser-Hahn, Mark Drewes, Simon Dörner-Rieping, Jan Dittgen, Martin Adamczewski
  • Patent number: 7956073
    Abstract: This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders.
    Type: Grant
    Filed: March 6, 2008
    Date of Patent: June 7, 2011
    Assignee: Array BioPharma Inc.
    Inventors: Jeremy Hans, Eli M. Wallace, Qian Zhao, Joseph P. Lyssikatos, Thomas D. Aicher, Ellen R Laird, John Robinson, Shelley Allen
  • Patent number: 7951523
    Abstract: In the liquid immersion lithography process, by simultaneously preventing deterioration of a resist film and deterioration of an immersion liquid employed during liquid immersion lithography which uses various immersion liquids, including water, resistance to post exposure delay of the resist film can be improved without increasing the number of processes, thereby making it possible to form a high resolution resist pattern using liquid immersion lithography. Using an alkaline soluble polymer, a crosslinking agent, and a solvent capable of dissolving them as at least constituent component, a composition is prepared and a protective film is formed on the surface of the resist film to be used, using the composition.
    Type: Grant
    Filed: July 29, 2005
    Date of Patent: May 31, 2011
    Assignee: Tokyo Ohka Kogyo Co., Ltd.
    Inventors: Keita Ishizuka, Kotaro Endo, Tomovuki Hiranoa
  • Patent number: 7947675
    Abstract: Compounds of the formula (I), in which the radicals R1 to R3 and AR are as defined in the description, processes for the preparation thereof, the use thereof in the treatment of cardiovascular diseases, and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: February 16, 2006
    Date of Patent: May 24, 2011
    Assignee: Merck Patent GmbH
    Inventors: Bruno Roux, Isabelle Berard
  • Publication number: 20110105572
    Abstract: This invention pertains to certain active carbamic acid compounds which inhibit HDAC activity and which have the following formula: wherein: A is a C5-20heteroaryl or C5-20carboaryl group and is optionally substituted; Q1 is a C2-7alkylene group having a backbone of at least 2 carbon atoms, and is optionally substituted; J is —N(R1)C(?O)— or —C(?O)N(R1)—; R1 is hydrogen, C1-7alkyl, C3-20heterocyclyl, or C5-20aryl; and, Q2 is C1-7alkylene, C5-20arylene, C5-20arylene-C1-7alkylene, or C1-7alkylene-C5-20arylene having a backbone of at least 3 carbon atoms, and is optionally substituted; and pharmaceutically acceptable salts thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit HDAC, and, e.g., to treat proliferative conditions, such as cancer and psoriasis.
    Type: Application
    Filed: January 4, 2011
    Publication date: May 5, 2011
    Inventors: Clare J. Watkins, Maria Rosario Romero-Martin, Kathryn G. Moore, James Ritchie, Paul W. Finn, Ivars Kalvinsh, Einars Loza, Igor Starchenkov, Klara Dikovska, Rasma M. Bokaldere, Vija Gailite, Maxim Vorona, Victor Andrianov, Daina Lolya, Valentina Semenikhina, Andris Amolins, C. John Harris, James E.S. Duffy
  • Patent number: 7919514
    Abstract: The invention relates to thiadiazole compounds useful for treating diseases mediated by protein kinase B (PKB). The invention also relates to the therapeutic use of such thiadiazole compounds and compositions thereof in treating disease states associated with abnormal cell growth, cancer, inflammation, and metabolic disorders.
    Type: Grant
    Filed: March 19, 2008
    Date of Patent: April 5, 2011
    Assignee: Amgen Inc.
    Inventors: Holger Monenschein, James Thomas Rider, Guomin Yao, Qingping Zeng
  • Patent number: 7910612
    Abstract: The present invention comprises 4-Oxy-N-[1,3,4]-thiadiazol-2-yl-benzene sulfonamides, the derivatives thereof and salts thereof as well as processes for their preparation and methods for their use as pharmaceutical compositions. More specifically, the invention relates to 4-oxy-N-[1,3,4]-thiadiazol-2-yl-benzene sulfonamides and to their physiologically acceptable salts and physiologically functional derivatives that exhibit peroxisome proliferator activator receptor (PPAR) PPARalpha, PPARdelta and PPARgamma agonist activity. The compounds themselves are defined by the structure of the formula I, wherein the various unnamed substituents are defined herein. The compounds are suitable for the treatment of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved as well as demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.
    Type: Grant
    Filed: April 4, 2008
    Date of Patent: March 22, 2011
    Assignee: Sanofi-Aventis
    Inventors: Stefanie Keil, Karl Schoenafinger, Hans Matter, Matthias Urmann, Maike Glien, Wolfgang Wendler, Hans-Ludwig Schaefer, Eugen Falk
  • Patent number: 7906546
    Abstract: The present invention relates to compounds of the formula (I) wherein R1, R2, R3, R4, R5, X1, X2, X3, X4, n, and k are defined in the description and claims, and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof. The compounds are useful for in the treatment and prophylaxis of diseases which are modulated by LXR? and/or LXR? agonists, including increased lipid and cholesterol levels, particularly low HDL-cholesterol, high LDL-cholesterol, atherosclerotic diseases, diabetes, particularly non-insulin dependent diabetes mellitus, metabolic syndrome, dyslipidemia, Alzheimer's disease, sepsis, inflammatory diseases such as colitis, pancreatitis, cholestasis/fibrosis of the liver, and diseases that have an inflammatory component such as Alzheimer's disease or impaired/improvable cognitive function.
    Type: Grant
    Filed: May 6, 2010
    Date of Patent: March 15, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Henrietta Dehmlow, Bernd Kuhn, Raffaello Masciadri, Narendra Panday, Hasane Ratni, Matthew Blake Wright
  • Patent number: 7902234
    Abstract: (wherein R1 and R4 are the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkynyl, substituted or unsubstituted lower alkenyl, or the like; R6 represents a substituted or unsubstituted heterocyclic group, substituted or unsubstituted aryl, or the like; R2 represents —C(?W)R6 or the like; R3 represents a hydrogen atom, —C(?WA)R6A, or the like) Antitumor agents which comprises a thiadiazoline derivative represented by the aforementioned general formula (I) or a pharmacologically acceptable salt thereof as an active ingredient are provided.
    Type: Grant
    Filed: June 2, 2010
    Date of Patent: March 8, 2011
    Assignees: Kyowa Hakko Kirin Co., Ltd., Fujifilm Corporation
    Inventors: Chikara Murakata, Kazuhiko Kato, Yoshihisa Ohta, Ryuichiro Nakai, Yoshinori Yamashita, Takeshi Takahashi
  • Patent number: 7879529
    Abstract: In the liquid immersion lithography process, by simultaneously preventing deterioration of a resist film and deterioration of an immersion liquid employed during liquid immersion lithography which uses various immersion liquids, including water, resistance to post exposure delay of the resist film can be improved without increasing the number of processes, thereby making it possible to form a high resolution resist pattern using liquid immersion lithography. Furthermore, it is possible to apply a high refractive index liquid immersion medium, used in combination with the high refractive index liquid immersion medium, thus making it possible to further improve pattern accuracy. Using a composition comprising an acrylic resin component having characteristics which have substantially no compatibility with a liquid in which a resist film is immersed, particularly water, and are also soluble in alkaline, a protective film is formed on the surface of a resist film used.
    Type: Grant
    Filed: July 29, 2005
    Date of Patent: February 1, 2011
    Assignee: Tokyo Ohka Kogyo Co., Ltd.
    Inventors: Kotaro Endo, Masaaki Yoshida, Keita Ishizuka
  • Patent number: 7875647
    Abstract: A heteroaryl-pyrazole compound of formula (I) or a pharmaceutically acceptable salt thereof is effective as a cannabinoid CB1 receptor inverse agonist or antagonist, which is useful for preventing or treating obesity and obesity-related metabolic disorders. The present invention also provides a method for preparing the inventive heteroaryl-pyrasole compounds or a pharmaceutically acceptable salt thereof, a pharmaceutical composition containing same, and a method for preventing or treating obesity and obesity-related metabolic disorders.
    Type: Grant
    Filed: September 28, 2007
    Date of Patent: January 25, 2011
    Assignee: Green Cross Corporation
    Inventors: Jinhwa Lee, Jeong Min Kim, Chong-Hwan Jonathan Chang, Suk Ho Lee, Hee Jeong Seo, Suk Youn Kang, Kwang-Seop Song, Jong Yup Kim, Min-ah Kim, Sung-han Lee, Kwang-Woo Ahn, Myung Eun Jung, Ji-Hyun Park
  • Publication number: 20110009386
    Abstract: A first aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof, wherein: one of R3 and R4 is H, and the other is selected from C1-6-alkyl, C1-6-haloalkyl, C1-6-alkoxy, and C6-12-aralkyl; or R3 and R4 are each independently selected from C1-6-alkyl and halo; R9 is a substituted 5 or 6-membered aryl or heteroaryl group or a 6,5- or 6,6-fused biaryl or heterobiaryl group. Compounds of formula (I) exhibit surprisingly high efficacies for human cathepsin S, excellent selectivity verses other mammalian cathepsins and are useful for treatment of diseases such as rheumatoid arthritis, multiple sclerosis, myasthenia gravis, transplant rejection, diabetes, Sjogrens syndrome, Grave's disease, systemic lupus erythematosis, osteoarthritis, psoriasis, idiopathic thrombocytopenic purpura, allergic rhinitis, asthma, atherosclerosis, obesity, chronic obstructive pulmonary disease and chronic pain.
    Type: Application
    Filed: August 9, 2010
    Publication date: January 13, 2011
    Applicant: Amura Therapeutics Limited
    Inventors: Martin Quibell, John P. Watts, Nicholas S. Flinn
  • Patent number: 7858645
    Abstract: The invention is concerned with novel indazole derivatives of formula (I) wherein R1, R2, R3, R4, R5, R6, X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used in the prevention or treatment of diseases which are modulated by L-CPT1 inhibitors.
    Type: Grant
    Filed: October 19, 2007
    Date of Patent: December 28, 2010
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jean Ackermann, Konrad Bleicher, Simona M. Ceccarelli, Odile Chomienne, Patrizio Mattei
  • Patent number: 7838023
    Abstract: The invention provides novel furoxan compounds, or pharmaceutically acceptable salts thereof, and novel compositions comprising at least one compound, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The compounds and compositions of the invention can also be bound to a matrix. The invention also provides methods for (a) treating cardiovascular diseases; (b) inhibiting platelet aggregation and platelet adhesion caused by the exposure of blood to a medical device; (c) treating pathological conditions resulting from abnormal cell proliferation; (d) treating transplantation rejections, (e) treating autoimmune, inflammatory, proliferative, hyperproliferative or vascular diseases; (f) reducing scar tissue or for inhibiting wound contraction; (g) treating diseases resulting from oxidative stress; (h) treating endothelial dysfunctions; and (j) treating diseases caused by endothelial dysfunctions.
    Type: Grant
    Filed: November 16, 2006
    Date of Patent: November 23, 2010
    Assignee: NitroMed, Inc.
    Inventors: David S. Garvey, Ramani R. Ranatunge
  • Patent number: 7812040
    Abstract: This invention is directed to a compound of the formula Ia or Ib, as defined herein, or a pharmaceutically acceptable salt thereof; a pharmaceutical composition containing a compound of formula I, a method of treatment of a disorder or condition that may be treated by antagonizing histamine H3 receptors, the method comprising administering to a mammal in need of such treatment a compound of formula I as described above, and a method of treatment of a disorder or condition selected from the group consisting of depression, mood disorders, schizophrenia, anxiety disorders, Alzheimer's disease, attention-deficit disorder (ADD), attention-deficit hyperactivity disorder (ADHD), psychotic disorders, sleep disorders, obesity, dizziness, epilepsy, motion sickness, respiratory diseases, allergy, allergy-induced airway responses, allergic rhinitis, nasal congestion, allergic congestion, congestion, hypotension, cardiovascular disease, diseases of the GI tract, hyper and hypo motility and acidic secretion of the gastro-i
    Type: Grant
    Filed: June 12, 2006
    Date of Patent: October 12, 2010
    Assignee: Pfizer Inc.
    Inventor: Travis T Wager
  • Publication number: 20100256115
    Abstract: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein X, Y, A, R1, R2, R3, R4, R4?, R5, R5?, R6 and R6? are as described herein.
    Type: Application
    Filed: March 18, 2010
    Publication date: October 7, 2010
    Inventors: Frederick Cohen, Kurt Deshayes, Wayne J. Fairbrother, Bainian Feng, John A. Flygare, Lewis J. Gazzard, Vickie Hsiao-Wei Tsui
  • Publication number: 20100249198
    Abstract: The present invention relates to a novel class of (R)-4-(heteroaryl)phenylpropionic derivatives of formula (I), useful in the inhibition of the chemotactic activation induced by the fraction C5a of complement. Said compounds are useful in the treatment of pathologies depending on the chemotactic activation of neutrophils and monocytes induced by the fraction C5a of the complement. In particular, the compounds of the invention are useful in the treatment of autoimmune hemolytic anemia (AIHA), psoriasis, bullous pemphigoid, rheumatoid arthritis, ulcerative colitis, acute respiratory distress syndrome, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of injury caused by ischemia and reperfusion.
    Type: Application
    Filed: October 17, 2008
    Publication date: September 30, 2010
    Applicant: Dompe S.p.A
    Inventors: Alessio Moriconi, Andrea Aramini
  • Publication number: 20100240622
    Abstract: The invention provides compositions and kits comprising at least one nitric oxide enhancing prostaglandin compound or a pharmaceutically acceptable salt thereof, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating ophthalmic disorders; (b) treating cerebrovascular disorders; (c) treating cardiovascular disorders; (d) treating benign prostatic hyperplasia (BPH); (e) treating peptic ulcers; (e) treating sexual dysfunctions and (f) inducing abortions. The nitric oxide enhancing prostaglandin compounds comprise at least one heterocyclic nitric oxide donor group and/or at least one nitroxide group.
    Type: Application
    Filed: March 19, 2007
    Publication date: September 23, 2010
    Applicant: NITROMED, INC.
    Inventor: David S. Garvey
  • Patent number: 7786311
    Abstract: The present invention is directed to novel 1,2,4-thiadiazol-2-ium derivatives useful as agonists or antagonists of the melanocortin receptor. More particularly, the compounds of the present invention are useful for the treatment of metabolic, CNS and dermatological disorders such as obesity, impaired oral glucose tolerance, elevated blood glucose levels, type II diabetes, Syndrome X, diabetic retinopathy, spinal cord injury, nerve injury, acute neurodegenerative disorders, chronic neurodegenerative disorders, plexopathies, male erectile dysfunction, dry eyes, acne, dry skin, aged skin, seborrheic dermatitis, rosacea, excessive ear wax, meibomian gland disorder, pseudofolliculitis, yeast infections, dandruff, hidradenitis suppurativa, ocular rosacea and eccrine gland disorder.
    Type: Grant
    Filed: August 5, 2008
    Date of Patent: August 31, 2010
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Magdalena Eisinger, Louis J. Fitzpatrick, Daniel H. Lee, Kevin Pan, Carlos Plata-Salaman, Allen B. Reitz, Virginia L. Smith-Swintosky, Boyu Zhao
  • Publication number: 20100210694
    Abstract: The present invention refers to new NO-donors aspirin derivatives, a process for their preparation and pharmaceutical compositions containing them.
    Type: Application
    Filed: September 3, 2008
    Publication date: August 19, 2010
    Applicant: NICOX S.A.
    Inventors: Roberta Fruttero, Alberto Gasco, Loretta Lazzarato, Monica Donnola, Barbara Rolando, Stefano Biondi
  • Publication number: 20100197644
    Abstract: Compounds of formula (I): The present invention relates to novel indazolyl ester or amide derivatives, to pharmaceutical compositions comprising such derivatives, to processes for preparing such novel derivatives and to the use of such derivatives as medicaments
    Type: Application
    Filed: December 21, 2009
    Publication date: August 5, 2010
    Inventors: Markus Berger, Jan Dahmén, Karl Edman, Anders Eriksson, Balint Gabos, Thomas Hansson, Martin Hemmerling, Krister Henriksson, Svetlana Ivanova, Matti Lepistö, Darren McKerrecher, Magnus Munck af Rosenschöld, Stinabritt Nilsson, Hartmut Rehwinkel, Camilla Taflin
  • Patent number: 7750088
    Abstract: The instant invention is an improved cure system composition and a method for curing chlorinated elastomer compositions. The cure system composition includes a polymercapto crosslinking agent, an inorganic base, and a quaternary ammonium salt. The quaternary ammonium salt has a formula selected from the group consisting of wherein R1 is an alkyl or aryl group containing between 4 and 12 carbon atoms; wherein R2 and R3 are independently alkyl or aryl groups containing between 1 and 8 carbon atoms; wherein the total number of carbon atoms on R2 and R3 are between 3 and 9; wherein R4 and R5 are methyl groups, and R6 is an alkyl group containing between 2 and 8 carbon atoms; and wherein X is an anion.
    Type: Grant
    Filed: March 10, 2006
    Date of Patent: July 6, 2010
    Assignee: Dow Global Technologies
    Inventors: Raymond L. Laakso, Jr., Gary R. Marchand
  • Publication number: 20100132856
    Abstract: A subject matter of the present invention is: the compounds of formula (I): in which: and Het is an azolyl radical: nitroazolyl or tetrazolyl; with the exception of 3-nitro-4-(4-nitro-1,2,3-triazol-1-yl)furazan; the preparation of said compounds; and the energetic compositions including at least one compound chosen from said compounds of formula (I) and 3-nitro-4-(4-nitro-1,2,3-triazol-1-yl)furazan.
    Type: Application
    Filed: January 15, 2008
    Publication date: June 3, 2010
    Applicant: SNPE MATERIAUX ENERGETIQUES
    Inventors: Guy Jacob, Gregoire Herve, Guy Cagnon, Frederic Alvarez
  • Patent number: 7723365
    Abstract: The present invention relates to oxadiazoles that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also relates to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
    Type: Grant
    Filed: August 15, 2005
    Date of Patent: May 25, 2010
    Assignees: Merck & Co., Inc., Merck Sharp & Dohme Corp.
    Inventors: Christopher D. Cox, Mark E. Fraley, Robert M. Garbaccio
  • Patent number: 7718678
    Abstract: Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof. X is N or N+O?, and Y is N or N+O?, provided that at least X or Y is N. The compounds are useful for the treatment of chemokine-mediated diseases such as COPD.
    Type: Grant
    Filed: June 27, 2006
    Date of Patent: May 18, 2010
    Assignee: Schering Corporation
    Inventor: Purakkattle J. Biju
  • Publication number: 20100113276
    Abstract: The use of N2-phenylamidines of formula (I) as herbicides is described. In this formula (I), R2, R3, R4, R5 and R6 are different radicals and A is a bond or various 1- or polyatomic bridging elements.
    Type: Application
    Filed: March 4, 2008
    Publication date: May 6, 2010
    Applicant: BAYER CROPSCIENCE AG
    Inventors: Birgit Kuhn, Harald Jakobi, Thomas Mueller, Joerg Tiebes, Heinz Kehne, Dirk Schmutzler, Martin Hills, Christopher Rosinger, Klaus Kunz, Mark Wilheim Drewes, Dieter Feucht, Thomas Seitz, Benoit Hartmann, Ralf Dunkel, Joerg Nico Greul, Oliver Guth, Kerstein Ilg, Darren James Mansfeld, Wahed Ahmed Moradi, Peter Dahmen, Ulrike Wachendorf-Neumann, Arnd Voerste, Dale Robert Mitchell, Jean-Pierre Andre Vors, Dale Robert Mitchell, Tom Hough
  • Patent number: 7678922
    Abstract: Provided herein are processes for the preparation of compounds useful for the treatment, prevention or management of diseases associated with a nonsense mutation. More specifically, provided herein are processes for the synthesis of 1,2,4-oxadiazoles. In particular, provided herein are processes useful for the preparation of 3-[5-(2-fluorophenyl)-[1,2,4]oxadiazol-3-yl]-benzoic acid.
    Type: Grant
    Filed: September 6, 2007
    Date of Patent: March 16, 2010
    Assignee: PTC Therapeutics, Inc.
    Inventors: Neil G. Almstead, Peter Seongwoo Hwang, Seemon Pines, Young-Choon Moon, James J. Takasugi
  • Patent number: 7659294
    Abstract: The present invention encompasses compounds of Formula I: as well as the pharmaceutically acceptable salts thereof. The compounds are S1P1/Edg1 receptor agonists and thus have immunosuppressive, anti-inflammatory and hemostatic activities by modulating leukocyte trafficking, sequestering lymphocytes in secondary lymphoid tissues, and enhancing vascular integrity. The invention is also directed to pharmaceutical compositions containing such compounds and methods of treatment or prevention.
    Type: Grant
    Filed: October 18, 2005
    Date of Patent: February 9, 2010
    Assignee: Merck & Co., Inc.
    Inventors: Jeffrey John Hale, Lin Yan
  • Publication number: 20100019169
    Abstract: This invention concerns the remote detection of threat clouds and evaluation of their components. Also included is the remote detection and evaluation of contamination on surfaces or in air streams. To enable this detection, fluorophores that are attached to POSS are used with two-photon LIF imaging that provides enhanced background-free imaging even in the presence of scattering particles such as dust, sand and water droplets.
    Type: Application
    Filed: January 25, 2008
    Publication date: January 28, 2010
    Applicant: Michigan Molecular Institute
    Inventor: Claire Hartmann-Thompson
  • Patent number: 7652049
    Abstract: Compounds having the structures of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis: In the compounds of Formula I, B or R2 is a phenyl group which has an ortho aryl, heterocyclic, benzoheterocyclic or benzocycloalkyl substituent, and one other position on the 5-membered ring has an aromatic, heterocyclic, cycloalkyl, benzoheterocyclic or benzocycloalkyl substituent connected directly to the ring or attached to the ring through a —CH2—.
    Type: Grant
    Filed: July 1, 2005
    Date of Patent: January 26, 2010
    Assignee: Merck & Co., Inc.
    Inventors: Amjad Ali, Joann M. Napolitano, Qiaolin Deng, Zhijian Lu, Peter J. Sinclair, Gayle E. Taylor, Christopher F. Thompson, Nazia Quraishi, Cameron J. Smith, Julianne A. Hunt, Adrian A. Dowst, Yi-Heng Chen, Hong Li
  • Publication number: 20100015178
    Abstract: The present invention is directed to 1,2,5-oxadiazole derivatives, and compositions of the same, which are inhibitors of indoleamine 2,3-dioxygenase and are useful in the treatment of cancer and other disorders, and to the processes and intermediates for making such 1,2,5-oxadiazole derivatives.
    Type: Application
    Filed: July 7, 2009
    Publication date: January 21, 2010
    Inventors: Andrew P. Combs, Eddy W. Yue, Richard B. Sparks, Wenyu Zhu, Jiacheng Zhou, Qiyan Lin, Lingkai Weng, Tai-Yuen Yue, Pingli Liu
  • Patent number: 7645882
    Abstract: To provide a inhibitor of protein modification products formation capable of inhibiting of vitamin B6 deficiency disease as a side effect, especially a renal protective agent. There is provided a use, as an active ingredient, of any of free or salt-form compounds of either of the formulae: (I) (II) [wherein R1 is substituted or unsubstituted aromatic ring; and each of R2, R3 and R4 is a hydrogen atom or monovalent organic group, or alternatively R2 and R3 cooperate to form a condensed ring or R3 and R4 cooperate to represent a divalent organic group, provided that R3 and R4 are not simultaneously hydrogen atoms].
    Type: Grant
    Filed: December 3, 2004
    Date of Patent: January 12, 2010
    Inventors: Toshio Miyata, Kiyoshi Kurokawa
  • Publication number: 20090326017
    Abstract: This invention discloses compositions and methods for inducing, promoting or otherwise facilitating pain relief. More particularly, the present invention discloses the use of sub-normovasodilatory doses of nitric oxide donors in the therapeutic management of vertebrate animals including humans, for the prevention or alleviation of pain, especially neuropathic pain. According to some embodiments of the present invention, nitric oxide donors are administered by any suitable route so as to provide concentrations of NO that are about ½ to 10?15 of those known to induce vasodilation in normal circulations.
    Type: Application
    Filed: June 29, 2009
    Publication date: December 31, 2009
    Applicant: THE UNIVERSITY OF QUEENSLAND
    Inventor: MAREE THERESE SMITH
  • Patent number: 7632851
    Abstract: The present invention relates to novel benzo[1,2,5]oxadiazoles and benzo[1,2,5]thiadiazoles of formula (I) wherein X is O or S, R1 is 5-(2-fluoro-ethylamino)-thiazol-2-yl, 5-(2-18F-ethylamino)-thiazol-2-yl or a group of formula (a) wherein Y is CH or N, R2 is NHCH3, NH11CH3, N(CH3)11CH3, N(CH3)2, N(11CH3)2, NH(CH2)nF, NH(CH2)n18F, N(CH3)(CH2)nF, N(CH3)—(CH2)n18F, O—(CH2)nF, O—(CH2)n18F, CONH(CH2)nF or CONH(CH2)n18F (n being in each case 2 to 4) and R3 is hydroxy, (C1-4)alkoxy, hydrogen or nitro, in free base or acid addition salt form; their preparation, their use as markers in diagnosis and compositions containing them.
    Type: Grant
    Filed: April 2, 2004
    Date of Patent: December 15, 2009
    Assignee: Novartis AG
    Inventors: Yves Auberson, Samuel Hintermann, Kaspar Zimmermann
  • Patent number: 7622475
    Abstract: The invention provides EP2 agonists, methods for their preparation, pharmaceutical compositions containing these compounds, and methods of using these compounds and compositions for lowering intraocular pressure and thereby treating glaucoma.
    Type: Grant
    Filed: July 27, 2007
    Date of Patent: November 24, 2009
    Assignee: Pfizer Inc
    Inventors: Ganesh Prasanna, Charles Floyd Bosworth, Jennifer Anne Lafontaine
  • Patent number: 7612149
    Abstract: The instant invention is an improved cure system composition and a method for curing chlorinated elastomer compositions. The cure system composition includes a polymercapto crosslinking agent, an inorganic base, and a quaternary ammonium salt. The quaternary ammonium salt has a formula selected from the group consisting of wherein R1 is an alkyl or aryl group containing between 4 and 12 carbon atoms; wherein R2 and R3 are independently alkyl or aryl groups containing between 1 and 8 carbon atoms; wherein the total number of carbon atoms on R2 and R3 are between 3 and 9; wherein R4 and R5 are methyl groups, and R6 is an alkyl group containing between 2 and 8 carbon atoms; and wherein X is an anion.
    Type: Grant
    Filed: March 10, 2006
    Date of Patent: November 3, 2009
    Assignee: Dow Global Technologies Inc.
    Inventors: Raymond L. Laakso, Jr., Gary R. Marchand
  • Patent number: 7585994
    Abstract: The invention relates to a method for producing perfluoroalkanesulfonic acid esters and for further transforming the same into the salts thereof. The invention also relates to the use of the produced compounds in electrolytes, batteries, capacitors, supercapacitors, and galvanic cells.
    Type: Grant
    Filed: May 31, 2006
    Date of Patent: September 8, 2009
    Assignee: Merck Patent GmbH
    Inventors: Nikolai Ignatyev, Michael Schmidt, Udo Heider, Peter Sartori, Andry Kucheryna
  • Publication number: 20090215225
    Abstract: Precursors for use in depositing tellurium-containing films on substrates such as wafers or other microelectronic device substrates, as well as associated processes of making and using such precursors, and source packages of such precursors. The precursors are useful for deposition of chalcogenide thin films in the manufacture of nonvolatile Phase Change Memory (PCM), by deposition techniques such as chemical vapor deposition (CVD) and atomic layer deposition (ALD).
    Type: Application
    Filed: February 24, 2009
    Publication date: August 27, 2009
    Applicant: ADVANCED TECHNOLOGY MATERIALS, INC.
    Inventors: Matthias Stender, Chongying Xu, Tianniu Chen, William Hunks, Philip S.H. Chen, Jeffrey F. Roeder, Thomas H. Baum
  • Patent number: 7576109
    Abstract: The present invention is directed to 1,3,4-oxadiazolones, compounds of formula I and their pharmaceutically acceptable salts stereoisomers, tautomers, or solvates thereof. Novel compounds include those of formula I, in which radicals are as defined herein. The compounds of this invention are modulators of PPARdelta and therefore useful as pharmaceutical agents, especially for the treatment of demyelinating diseases and disorders of fatty acid metabolism and glucose utilization.
    Type: Grant
    Filed: September 26, 2006
    Date of Patent: August 18, 2009
    Assignees: Aventis Pharmaceuticals Inc., Sanofi-Aventis Deutschland GmbH
    Inventors: Daniel G. McGarry, Karen Chandross, Jean Merrill, Jochen Goerlitzer, Stefanie Keil, Wolfgang Wendler, Patrick Bernardelli
  • Patent number: 7572820
    Abstract: This invention relates to non-steroidal compounds that are modulators of androgen receptor, and also to the methods for the making and use of such compounds.
    Type: Grant
    Filed: September 27, 2007
    Date of Patent: August 11, 2009
    Assignee: SmithKline Beecham Corporation
    Inventors: Philip Stewart Turnbull, Rodolfo Cadilla, Andrew Larkin, Huiquiang Zhou, Eugene L. Stewart, Katherine Stetson, Darryl Lynn McDougald, Amarjit Sab Randhawa, John A. Ray
  • Patent number: 7572816
    Abstract: The present invention is directed to compounds having the structure wherein R1, R2, R3, R4, R5 and m are as defined herein. The compounds of this invention are novel therapeutic agents for the treatment of cancer, metabolic diseases and skin disorders in mammalian subjects. These compounds are also useful modulators of gene expression. They exert their activity by interfering with certain cellular signal transduction cascades. The compounds of the invention are thus also useful for regulating cell differentiation and cell cycle processes that are controlled or regulated by various hormones or cytokines. In particular, the invention relates to compounds that induce apoptosis of cancer cells and therefore may be used for the treatment or prevention of cancer, including advanced cancers and pre-cancerous cells.
    Type: Grant
    Filed: July 21, 2004
    Date of Patent: August 11, 2009
    Assignee: Auspex Pharmaceuticals, Inc.
    Inventors: Bruno Tse, Sepehr Sarshar
  • Publication number: 20090170911
    Abstract: Azole compounds represented by formula I: wherein ring A is isoxazole and the like, R1 is a substituted or unsubstituted aryl group and the like, R2 is a hydrogen atom and the like, and R3 is a substituted or unsubstituted alkyl group and the like, and pharmaceutically acceptable salts thereof inhibit the physiological activity of lysophosphatidic acid (LPA), and are useful as for the prophylaxis or treatment of diseases in which inhibition of the physiological activity of LPA is useful for the prophylaxis or treatment thereof, such as diseases involving the LPA receptor.
    Type: Application
    Filed: February 20, 2009
    Publication date: July 2, 2009
    Applicant: AJINOMOTO CO. INC
    Inventors: Takashi YAMAMOTO, Akira Chiba, Koichi Fujita, Yuka Kataba, Koji Ohsumi, Sayaka Asari, Naoyuki Fukuchi, Misato Noguchi, Itsuya Tanabe, Chiori Ijichi, Naoko Oomuta, Yuko Iida, Satoshi Iwayama
  • Patent number: 7553964
    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: June 1, 2006
    Date of Patent: June 30, 2009
    Assignee: Abbott Laboratories
    Inventors: Huaqing Liu, Kathryn J. Hancock, legal representative, Marlon D. Cowart, Arthur A. Hancock
  • Publication number: 20090137816
    Abstract: This invention consists of a method for converting diaminoglyoxime to diaminofurazan that can be carried out efficiently at about atmospheric pressure without the need for high pressure containment apparatus. This invention also consists of a method which comprises converting diaminoglyoxime to diaminofurazan at about atmospheric pressure in the presence of a strong base and/or an organic polar solvent.
    Type: Application
    Filed: December 15, 2000
    Publication date: May 28, 2009
    Inventors: Kurt Baum, Abdollah Bashir-Hashemi
  • Publication number: 20090130077
    Abstract: The invention relates to substituted benzothiazoles, benzoxazoles—and their counterparts having pyridine and pyrimidine rings replacing the benzene ring—that are PDE4 inhibitors useful for treating stroke, myocardial infarct, and cardiovascular inflammatory conditions, to pharmaceutical compositions comprising these compounds, and to methods for the treatment of stroke, myocardial infarct, and cardiovascular inflammatory conditions in a mammal. The compounds have general formula I: in which A and B are carbocycles or heterocycles.
    Type: Application
    Filed: November 20, 2008
    Publication date: May 21, 2009
    Applicant: deCODE genetics ehf
    Inventors: Jasbir Singh, Mark E. Gurney, Alex Burgin, Vincent Sandanayaka, Alexander Kiselyov, Munagala Rao
  • Patent number: 7528137
    Abstract: Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.
    Type: Grant
    Filed: October 27, 2005
    Date of Patent: May 5, 2009
    Assignees: Cytokinetics, Inc., SmithKline Beecham Corporation
    Inventors: Bainian Feng, Gustave Bergnes, David J. Morgans, Jr., Dashyant Dhanak, Steven David Knight, Michael Gerard Darcy
  • Patent number: 7514459
    Abstract: Compounds of formula I: are potent inhibitors of gamma-secretase and hence find use in treatment or prevention of diseases associated with deposition of ?-amyloid.
    Type: Grant
    Filed: September 16, 2004
    Date of Patent: April 7, 2009
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Ian James Collins, Joanne Clare Hannam, Andrew Madin, Mark Peter Ridgill
  • Patent number: 7514434
    Abstract: The present invention relates to substituted diphenyl heterocycle compounds having an oxadiazole moiety and pharmaceutical compositions thereof that inhibit replication of HCV virus. The present invention also relates to the use of the compounds and/or compositions to inhibit HCV replication and/or proliferation and to treat or prevent HCV infections.
    Type: Grant
    Filed: February 22, 2005
    Date of Patent: April 7, 2009
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Dane Goff, Rajinder Singh, Henry Lu
  • Publication number: 20090082393
    Abstract: Compounds of formula (I): (A)m·(B)n??(I) wherein A represents an angiotensin-converting enzyme inhibitor compound containing at least one salt-forming basic function, B represents a compound containing at least one salt-forming acid function and at least one NO donor group, m represents the number of acid functions of B that have been converted to a salt and n represents the number of basic functions of A that have been converted to a salt, the bond or bonds between A and B being of the ionic type. Medicinal products containing the same which are useful in treating cardiovascular pathologies.
    Type: Application
    Filed: September 17, 2008
    Publication date: March 26, 2009
    Applicant: LES LABORATOIRES SERVIER
    Inventors: Guillaume De Nanteuil, Bernard Portevin, Philippe Gloanec, Jean-Gilles Parmentier, Alain Benoist, Tony Verbeuren, Alain Rupin, Christine Courchay, Serge Simonet
  • Patent number: 7504520
    Abstract: The present invention is directed to compounds of formula (I) wherein variables W, X, Y, D, A, n, R1, R2 and R9 are as defined in the description.
    Type: Grant
    Filed: May 10, 2006
    Date of Patent: March 17, 2009
    Assignee: Abbott Laboratories
    Inventors: Arthur Gomtsyan, Richard J. Perner, John R. Koenig, Margaret Chi-Ping Hsu, Dilinie P. Fernando, Chih-Hung Lee